Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
44570962 190636 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 435 4 1 5 2.5 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL480821 190636 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 435 4 1 5 2.5 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
145950336 169606 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 3 3 3.1 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4172656 169606 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 3 3 3.1 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.8b00322
156016416 184436 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 6 3 5 3.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641513 184436 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 6 3 5 3.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
16752684 101274 1 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 484 5 1 7 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL251572 101274 1 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 484 5 1 7 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
156014430 184002 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4635542 184002 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
156016416 184436 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 6 3 5 3.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641513 184436 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 6 3 5 3.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
16752684 101274 1 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 484 5 1 7 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2008.12.042
CHEMBL251572 101274 1 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 484 5 1 7 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2008.12.042
44570963 190659 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 435 4 1 5 2.5 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL481013 190659 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 435 4 1 5 2.5 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
156014430 184002 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4635542 184002 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
44444563 161734 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 478 5 1 6 3.7 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)cc1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL401134 161734 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 478 5 1 6 3.7 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)cc1)CC2 10.1016/j.bmcl.2007.09.067
156011926 184179 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 6 4 5 2.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4638297 184179 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 6 4 5 2.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
44571002 197877 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 437 4 2 6 1.1 Cc1ccc(-c2ccc(S(=O)(=O)N3CC[C@H](O)[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL518774 197877 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 437 4 2 6 1.1 Cc1ccc(-c2ccc(S(=O)(=O)N3CC[C@H](O)[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
44449987 102668 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 493 16 4 10 0.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCSCCO 10.1016/j.bmcl.2008.03.059
CHEMBL259166 102668 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 493 16 4 10 0.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCSCCO 10.1016/j.bmcl.2008.03.059
25010378 166177 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 525 16 4 11 -0.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCS(=O)(=O)CCO 10.1016/j.bmcl.2008.03.059
CHEMBL410074 166177 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 525 16 4 11 -0.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCS(=O)(=O)CCO 10.1016/j.bmcl.2008.03.059
44449955 166191 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 509 14 4 9 1.6 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1cccc(O)c1 10.1016/j.bmcl.2008.03.059
CHEMBL410085 166191 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 509 14 4 9 1.6 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1cccc(O)c1 10.1016/j.bmcl.2008.03.059
156011926 184179 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 6 4 5 2.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4638297 184179 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 6 4 5 2.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
156017918 184585 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 591 7 3 7 2.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4643530 184585 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 591 7 3 7 2.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2Cl)on1 10.1021/acs.jmedchem.0c00828
156015100 184351 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4640507 184351 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
156017918 184585 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 591 7 3 7 2.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4643530 184585 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 591 7 3 7 2.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2Cl)on1 10.1021/acs.jmedchem.0c00828
44570960 190767 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 417 4 1 5 2.4 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2)o1 10.1016/j.bmcl.2008.12.042
CHEMBL481796 190767 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 417 4 1 5 2.4 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2)o1 10.1016/j.bmcl.2008.12.042
24894012 183576 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 497 14 4 9 1.6 CC(C)(N)C(=O)N[C@H](CCC(F)(F)c1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.05.100
CHEMBL460680 183576 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 497 14 4 9 1.6 CC(C)(N)C(=O)N[C@H](CCC(F)(F)c1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.05.100
156015100 184351 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4640507 184351 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
44437979 17099 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 655 12 5 5 4.1 NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)c1ccccc1 10.1016/j.bmc.2007.01.057
CHEMBL1162065 17099 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 655 12 5 5 4.1 NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)c1ccccc1 10.1016/j.bmc.2007.01.057
44437979 17099 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 655 12 5 5 4.1 NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)c1ccccc1 10.1016/j.bmc.2007.01.057
CHEMBL1162065 17099 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 655 12 5 5 4.1 NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)c1ccccc1 10.1016/j.bmc.2007.01.057
44454303 104345 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
CHEMBL270666 104345 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
156020725 184884 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647963 184884 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
44570764 190828 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 481 4 1 4 3.8 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3cc(Cl)ccc3Cl)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL482220 190828 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 481 4 1 4 3.8 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3cc(Cl)ccc3Cl)cc2)C1 10.1016/j.bmcl.2008.12.042
24803512 95782 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1Cl 10.6019/CHEMBL2364335
CHEMBL2364468 95782 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1Cl 10.6019/CHEMBL2364335
156020725 184884 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647963 184884 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
9917957 116495 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Compound was evaluated for GH release for effect on human GH secretagogue receptorCompound was evaluated for GH release for effect on human GH secretagogue receptor
ChEMBL 683 14 4 5 4.3 NC(=O)CN(CCc1ccccc1)C(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1 10.1021/jm970342o
CHEMBL322912 116495 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Compound was evaluated for GH release for effect on human GH secretagogue receptorCompound was evaluated for GH release for effect on human GH secretagogue receptor
ChEMBL 683 14 4 5 4.3 NC(=O)CN(CCc1ccccc1)C(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1 10.1021/jm970342o
44447855 201635 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 539 15 4 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1-c1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL539929 201635 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 539 15 4 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1-c1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
178024 8752 33 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
5867 8752 33 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
CHEMBL13817 8752 33 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
156013414 184251 6 None 1905 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4639111 184251 6 None 1905 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
156013297 184263 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639229 184263 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
44452749 102990 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 499 7 2 6 4.5 COc1ccc(F)c(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)cc2)c1 10.1016/j.bmcl.2007.12.021
CHEMBL260819 102990 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 499 7 2 6 4.5 COc1ccc(F)c(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)cc2)c1 10.1016/j.bmcl.2007.12.021
44570765 198219 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 421 4 1 5 2.1 Cc1ccc(-c2ccc(S(=O)(=O)N3CCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL519301 198219 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 421 4 1 5 2.1 Cc1ccc(-c2ccc(S(=O)(=O)N3CCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
59007047 95740 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 6 5.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)cc1C 10.6019/CHEMBL2364335
CHEMBL2364427 95740 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 6 5.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)cc1C 10.6019/CHEMBL2364335
178024 8752 33 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
5867 8752 33 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
CHEMBL13817 8752 33 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
25022640 104577 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
CHEMBL271876 104577 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
44454337 162382 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL404545 162382 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
44447839 101766 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 499 14 4 10 0.6 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)cc1F)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254765 101766 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 499 14 4 10 0.6 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)cc1F)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
156013414 184251 6 None 1905 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4639111 184251 6 None 1905 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
156013297 184263 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639229 184263 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
44447857 173655 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 497 14 4 10 0.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1Cl)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL428592 173655 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 497 14 4 10 0.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1Cl)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
156019724 184770 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4646219 184770 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
22888474 70238 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 525 9 1 6 5.6 COc1cccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)c1 10.1016/j.bmcl.2005.02.040
CHEMBL179823 70238 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 525 9 1 6 5.6 COc1cccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)c1 10.1016/j.bmcl.2005.02.040
11306502 70416 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180094 70416 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
11306502 70416 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180094 70416 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
11306502 70416 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180094 70416 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
22888476 129596 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 525 9 1 6 5.6 COc1ccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
CHEMBL360547 129596 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 525 9 1 6 5.6 COc1ccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
22888476 129596 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 525 9 1 6 5.6 COc1ccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
CHEMBL360547 129596 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 525 9 1 6 5.6 COc1ccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
44454117 162335 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
CHEMBL404336 162335 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
44444559 101211 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 451 4 1 5 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc3ccccc3c1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL251169 101211 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 451 4 1 5 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc3ccccc3c1)CC2 10.1016/j.bmcl.2007.09.067
156011750 184069 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccccc2Cl)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4636502 184069 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccccc2Cl)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
156019724 184770 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4646219 184770 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
44453123 104762 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 503 6 2 5 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(Cl)ccc2F)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL272753 104762 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 503 6 2 5 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(Cl)ccc2F)cc1 10.1016/j.bmcl.2007.12.021
44570966 190348 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 437 4 2 6 1.1 Cc1ccc(-c2ccc(S(=O)(=O)N3C[C@H](O)C[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL480037 190348 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 437 4 2 6 1.1 Cc1ccc(-c2ccc(S(=O)(=O)N3C[C@H](O)C[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
59007062 95742 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)cc1F 10.6019/CHEMBL2364335
CHEMBL2364429 95742 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)cc1F 10.6019/CHEMBL2364335
24803514 95787 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1Cl 10.6019/CHEMBL2364335
CHEMBL2364472 95787 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1Cl 10.6019/CHEMBL2364335
44447852 162341 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 477 14 4 10 0.6 Cc1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL404354 162341 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 477 14 4 10 0.6 Cc1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
156011750 184069 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccccc2Cl)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4636502 184069 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccccc2Cl)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
44450016 167339 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 489 17 4 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL411259 167339 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 489 17 4 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCCCO 10.1016/j.bmcl.2008.03.059
44454367 102036 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
CHEMBL256235 102036 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
22867441 17087 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161835 17087 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1016/j.bmc.2007.01.057
16114096 85935 1 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)c(OC)c1 10.1021/jm0704550
CHEMBL2113324 85935 1 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)c(OC)c1 10.1021/jm0704550
22867441 17087 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161835 17087 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1016/j.bmc.2007.01.057
44447841 161857 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.6 CC(C)(N)C(=O)N[C@H](COCc1cccc(Cl)c1Cl)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL401827 161857 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.6 CC(C)(N)C(=O)N[C@H](COCc1cccc(Cl)c1Cl)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
69195371 95666 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 472 6 2 7 4.1 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)n3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364354 95666 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 472 6 2 7 4.1 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)n3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
44450101 166239 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 495 13 4 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCNC(=O)CCc1cccc(O)c1 10.1016/j.bmcl.2008.03.059
CHEMBL410135 166239 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 495 13 4 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCNC(=O)CCc1cccc(O)c1 10.1016/j.bmcl.2008.03.059
44391039 138566 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 540 9 1 7 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3cccc([N+](=O)[O-])c3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL369329 138566 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 540 9 1 7 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3cccc([N+](=O)[O-])c3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44449988 167880 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 477 16 4 10 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCOCCO 10.1016/j.bmcl.2008.03.059
CHEMBL411697 167880 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 477 16 4 10 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCOCCO 10.1016/j.bmcl.2008.03.059
44447843 101795 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1C(F)(F)F)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254973 101795 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1C(F)(F)F)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
10280020 69866 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 529 8 1 5 6.2 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccc(Cl)cc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL178900 69866 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 529 8 1 5 6.2 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccc(Cl)cc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
156021297 184868 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647797 184868 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44444571 100754 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 498 5 1 7 4.1 COc1cc2c(cc1N1C[C@H](C)NC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL248544 100754 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 498 5 1 7 4.1 COc1cc2c(cc1N1C[C@H](C)NC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
10553921 111337 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 517 9 4 4 2.9 CCNC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
CHEMBL310457 111337 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 517 9 4 4 2.9 CCNC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
10345516 146053 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1016/j.bmc.2007.01.057
CHEMBL379074 146053 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1016/j.bmc.2007.01.057
156012122 184160 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637980 184160 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156021297 184868 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647797 184868 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
11584048 104805 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1Cl 10.1016/j.bmcl.2007.12.021
CHEMBL272993 104805 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1Cl 10.1016/j.bmcl.2007.12.021
24755624 164079 2 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL407706 164079 2 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1 10.1016/j.bmcl.2007.12.021
24755624 164079 2 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1 10.1016/j.bmcl.2008.12.042
CHEMBL407706 164079 2 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1 10.1016/j.bmcl.2008.12.042
69197353 95720 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(NS(=O)(=O)c2ccc(-c3cc(C)cs3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364408 95720 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(NS(=O)(=O)c2ccc(-c3cc(C)cs3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
44454060 162111 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL403180 162111 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
10553921 111337 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 517 9 4 4 2.9 CCNC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
CHEMBL310457 111337 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 517 9 4 4 2.9 CCNC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
10345516 146053 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1016/j.bmc.2007.01.057
CHEMBL379074 146053 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1016/j.bmc.2007.01.057
127047525 146545 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 858 20 7 9 5.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798559 146545 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 858 20 7 9 5.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
156022162 184985 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 8 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)NC[C@@H]1CCCN1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4649634 184985 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 8 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)NC[C@@H]1CCCN1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
156012122 184160 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637980 184160 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
20600693 70230 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 566 11 1 6 4.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C(=O)N(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL179785 70230 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 566 11 1 6 4.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C(=O)N(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44560945 185881 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 391 9 2 7 2.1 CC(C)(N)C(=O)N[C@H](CCC(F)(F)c1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.05.100
CHEMBL471751 185881 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 391 9 2 7 2.1 CC(C)(N)C(=O)N[C@H](CCC(F)(F)c1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.05.100
216208 16499 33 None -5 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
CHEMBL113313 16499 33 None -5 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
44449891 103249 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 539 16 4 10 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1ccccc1C(=O)NCCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL262358 103249 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 539 16 4 10 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1ccccc1C(=O)NCCCCO 10.1016/j.bmcl.2008.03.059
216208 16499 33 None -5 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
CHEMBL113313 16499 33 None -5 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
156021478 184834 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 7 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647258 184834 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 7 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3)cc2c1 10.1021/acs.jmedchem.0c00828
44437955 17097 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 534 11 4 6 2.6 NCC(O)CNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCCN1C(=O)CCSc2ccccc21 10.1016/j.bmc.2007.01.057
CHEMBL1162063 17097 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 534 11 4 6 2.6 NCC(O)CNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCCN1C(=O)CCSc2ccccc21 10.1016/j.bmc.2007.01.057
9807597 189796 5 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 513 7 4 4 3.5 CNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1016/j.bmc.2007.01.057
CHEMBL47938 189796 5 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 513 7 4 4 3.5 CNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1016/j.bmc.2007.01.057
156018364 184692 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645148 184692 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156021478 184834 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 7 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647258 184834 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 7 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3)cc2c1 10.1021/acs.jmedchem.0c00828
156022090 184982 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4649603 184982 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
156022162 184985 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 8 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)NC[C@@H]1CCCN1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4649634 184985 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 8 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)NC[C@@H]1CCCN1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
56926175 75788 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL1923504 75788 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
56926356 75794 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O nan
CHEMBL1923512 75794 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O nan
56926461 75811 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923609 75811 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926462 75812 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923610 75812 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
57399248 75819 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923617 75819 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
11664206 75828 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923626 75828 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
56926894 75839 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
CHEMBL1923638 75839 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
11526745 75843 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923642 75843 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C nan
11526696 78377 17 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
CHEMBL1923502 78377 17 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
CHEMBL1963249 78377 17 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
134130631 149151 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 576 5 4 6 3.4 COc1ccc(C[C@@H]2NC(=O)C3(CCCC3)NC(=O)[C@H](CC(C)C)NCCOc3ccccc3/C=C\CNC2=O)cc1 nan
CHEMBL3889512 149151 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 576 5 4 6 3.4 COc1ccc(C[C@@H]2NC(=O)C3(CCCC3)NC(=O)[C@H](CC(C)C)NCCOc3ccccc3/C=C\CNC2=O)cc1 nan
134137202 149604 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 552 5 3 6 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3893048 149604 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 552 5 3 6 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134137257 149915 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 540 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3895776 149915 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 540 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134133518 150231 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 552 2 4 5 3.4 CC1(C)NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
CHEMBL3898348 150231 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 552 2 4 5 3.4 CC1(C)NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
134133352 150283 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3898794 150283 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@@H](C)N(C)C1=O nan
134134286 150472 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 598 5 3 5 4.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3900284 150472 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 598 5 3 5 4.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134135712 150916 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 533 4 4 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN(C)C1=O nan
CHEMBL3903845 150916 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 533 4 4 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN(C)C1=O nan
11512561 151147 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 574 3 3 5 3.4 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2Cl)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3905791 151147 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 574 3 3 5 3.4 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2Cl)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134133037 151345 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3907497 151345 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](C)N(C)C1=O nan
134132893 151641 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 4 4 6 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3909834 151641 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 4 4 6 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134132152 151710 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3910300 151710 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@@H](C)N(C)C1=O nan
134142218 152065 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 564 4 4 5 3.5 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3913052 152065 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 564 4 4 5 3.5 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)C2(CCCC2)NC1=O nan
134142433 152104 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 534 3 4 6 1.8 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOC2)NC1=O nan
CHEMBL3913335 152104 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 534 3 4 6 1.8 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOC2)NC1=O nan
134142839 152164 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3913855 152164 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134143635 152352 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2Cl)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3915269 152352 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2Cl)NC(=O)C2(CCCC2)NC1=O nan
134143366 152538 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 578 4 4 4 4.6 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3916659 152538 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 578 4 4 4 4.6 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134142204 152715 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3918046 152715 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
11584702 152969 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 540 3 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3920049 152969 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 540 3 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134140270 153151 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 536 4 3 5 3.1 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3921499 153151 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 536 4 3 5 3.1 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134139279 153225 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 594 4 4 5 4.1 CCC(C)[C@H]1NCCOc2ccccc2[C@H]2C[C@@H]2CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3922056 153225 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 594 4 4 5 4.1 CCC(C)[C@H]1NCCOc2ccccc2[C@H]2C[C@@H]2CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134139286 153332 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3922810 153332 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
134141886 153896 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 546 4 4 5 3.4 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3927481 153896 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 546 4 4 5 3.4 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
117812380 154530 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 617 5 4 7 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(NS(C)(=O)=O)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3932408 154530 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 617 5 4 7 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(NS(C)(=O)=O)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134138595 154533 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 544 2 4 5 3.3 O=C1NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccccc1 nan
CHEMBL3932434 154533 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 544 2 4 5 3.3 O=C1NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccccc1 nan
134138824 154793 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 525 3 3 6 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ncccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3934402 154793 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 525 3 3 6 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ncccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134148504 155133 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 518 4 3 4 3.4 CC[C@H](C)[C@@H]1NCc2ccccc2C/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3937200 155133 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 518 4 3 4 3.4 CC[C@H](C)[C@@H]1NCc2ccccc2C/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134149306 155253 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 3 3 5 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCC#Cc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3938104 155253 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 3 3 5 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCC#Cc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134145791 155565 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 596 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2c(F)c(F)c(F)c(F)c2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3940705 155565 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 596 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2c(F)c(F)c(F)c(F)c2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134145564 155869 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 518 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3943086 155869 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 518 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134147441 156268 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 2 4 5 3.0 C[C@H]1NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
CHEMBL3946348 156268 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 2 4 5 3.0 C[C@H]1NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
134155239 157793 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 564 3 4 5 3.4 O=C1NC/C=C\c2ccccc2OCCN[C@@H](C2CC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccc(Cl)cc1 nan
CHEMBL3958460 157793 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 564 3 4 5 3.4 O=C1NC/C=C\c2ccccc2OCCN[C@@H](C2CC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccc(Cl)cc1 nan
134155132 157871 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 502 4 3 5 2.9 CC[C@H](C)[C@]1(C)NCCOc2ccccc2CCCNC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3959108 157871 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 502 4 3 5 2.9 CC[C@H](C)[C@]1(C)NCCOc2ccccc2CCCNC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](C)N(C)C1=O nan
134154079 159182 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 512 4 4 5 3.2 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](CC(C)C)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3970499 159182 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 512 4 4 5 3.2 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](CC(C)C)NC(=O)C2(CCCC2)NC1=O nan
134153247 159499 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 582 4 4 6 2.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCOC2)NC1=O nan
CHEMBL3973085 159499 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 582 4 4 6 2.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCOC2)NC1=O nan
44570763 197038 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 449 4 1 4 2.7 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3cc(F)ccc3F)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL517543 197038 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 449 4 1 4 2.7 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3cc(F)ccc3F)cc2)C1 10.1016/j.bmcl.2008.12.042
9890504 96515 0 None - 1 Human 9.0 pEC50 = 9 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 461 10 3 10 -0.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)N1CC[C@@H](O)C1 10.1021/jm7010595
CHEMBL237699 96515 0 None - 1 Human 9.0 pEC50 = 9 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 461 10 3 10 -0.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)N1CC[C@@H](O)C1 10.1021/jm7010595
24969109 95650 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 444 5 2 6 3.8 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cccc(N4C[C@H](C)N[C@H](C)C4)n3)cc2F)o1 10.6019/CHEMBL2364335
CHEMBL2364338 95650 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 444 5 2 6 3.8 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cccc(N4C[C@H](C)N[C@H](C)C4)n3)cc2F)o1 10.6019/CHEMBL2364335
11518200 95665 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364353 95665 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11641108 95694 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364382 95694 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69197887 95715 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2C)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364403 95715 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2C)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
44447856 168593 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 558 15 4 12 1.6 Cc1noc(C)c1-c1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL414394 168593 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 558 15 4 12 1.6 Cc1noc(C)c1-c1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
156018364 184692 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645148 184692 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156022090 184982 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4649603 184982 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
10323604 17081 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161828 17081 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
10323604 17081 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161828 17081 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
44447853 101739 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 493 15 4 11 0.3 COc1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254565 101739 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 493 15 4 11 0.3 COc1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
25022503 162342 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 540 15 4 11 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1-c1cccnc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL404355 162342 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 540 15 4 11 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1-c1cccnc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44269035 34105 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 490 5 4 5 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CC(O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
CHEMBL13675 34105 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 490 5 4 5 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CC(O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
44269039 105117 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@@]2(CC(=O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
CHEMBL275093 105117 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@@]2(CC(=O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
145956061 169472 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4170481 169472 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
44570965 196616 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 418 4 2 6 0.8 Cc1ccc(-c2ccc(S(=O)(=O)N3CCNC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2)o1 10.1016/j.bmcl.2008.12.042
CHEMBL516602 196616 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 418 4 2 6 0.8 Cc1ccc(-c2ccc(S(=O)(=O)N3CCNC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2)o1 10.1016/j.bmcl.2008.12.042
69194933 95737 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 455 5 2 5 5.0 Cc1csc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3C)cc2)c1 10.6019/CHEMBL2364335
CHEMBL2364424 95737 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 455 5 2 5 5.0 Cc1csc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3C)cc2)c1 10.6019/CHEMBL2364335
69198297 95746 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cc(C)cs3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364432 95746 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cc(C)cs3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
44447850 101710 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 488 14 4 11 0.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1C#N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254363 101710 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 488 14 4 11 0.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1C#N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44450015 103093 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 475 16 4 9 0.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL261358 103093 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 475 16 4 9 0.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCCO 10.1016/j.bmcl.2008.03.059
178024 8752 33 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/j.bmc.2007.01.057
5867 8752 33 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/j.bmc.2007.01.057
CHEMBL13817 8752 33 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/j.bmc.2007.01.057
178024 8752 33 None 1 3 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(97)10199-8
5867 8752 33 None 1 3 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(97)10199-8
CHEMBL13817 8752 33 None 1 3 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(97)10199-8
178024 8752 33 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/j.bmc.2007.01.057
5867 8752 33 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/j.bmc.2007.01.057
CHEMBL13817 8752 33 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/j.bmc.2007.01.057
145956061 169472 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4170481 169472 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
44450104 102576 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 496 14 4 10 -1.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCS(N)(=O)=O 10.1016/j.bmcl.2008.03.059
CHEMBL258761 102576 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 496 14 4 10 -1.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCS(N)(=O)=O 10.1016/j.bmcl.2008.03.059
CHEMBL500468 220894 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/j.bmcl.2008.03.059
CHEMBL500468 220894 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1021/jm300414b
22888475 70599 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 523 9 1 6 5.4 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccc(C=O)cc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180246 70599 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 523 9 1 6 5.4 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccc(C=O)cc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL500468 220894 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/j.bmcl.2005.02.040
162653916 187324 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 707 15 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4753794 187324 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 707 15 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL500468 220894 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/j.bmcl.2008.02.021
CHEMBL500468 220894 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/j.bmcl.2008.05.100
178024 8752 33 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(01)00324-9
5867 8752 33 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(01)00324-9
CHEMBL13817 8752 33 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(01)00324-9
156012849 184077 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4636571 184077 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44390996 71078 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 563 8 1 5 6.6 CC(C)N(CCNC(=O)C1c2ccc(Oc3cccc(C(F)(F)F)c3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181063 71078 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 563 8 1 5 6.6 CC(C)N(CCNC(=O)C1c2ccc(Oc3cccc(C(F)(F)F)c3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
11353414 71390 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 553 11 1 7 4.5 COC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181764 71390 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 553 11 1 7 4.5 COC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
11353414 71390 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 553 11 1 7 4.5 COC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181764 71390 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 553 11 1 7 4.5 COC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44347919 23145 0 None - 1 Rat 8.8 pEC50 = 8.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 606 14 3 6 4.2 C[C@H](O)CNC(=O)[C@@H](Cc1cccs1)N(C)C(=O)[C@@H](CC1=CCC(c2ccccc2)C=C1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL122939 23145 0 None - 1 Rat 8.8 pEC50 = 8.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 606 14 3 6 4.2 C[C@H](O)CNC(=O)[C@@H](Cc1cccs1)N(C)C(=O)[C@@H](CC1=CCC(c2ccccc2)C=C1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
16133832 220110 18 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/acs.jmedchem.8b01644
CHEMBL425281 220110 18 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/acs.jmedchem.8b01644
145957574 169080 0 None 57 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164328 169080 0 None 57 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
9875705 212080 1 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
CHEMBL79263 212080 1 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
156012849 184077 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4636571 184077 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156013219 184268 0 None 60 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639379 184268 0 None 60 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
11648350 95693 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3ccsc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364381 95693 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3ccsc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
59007043 95696 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2c(Cl)cccc2c1 10.6019/CHEMBL2364335
CHEMBL2364384 95696 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2c(Cl)cccc2c1 10.6019/CHEMBL2364335
69197106 95739 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(C)s3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364426 95739 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(C)s3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
24803348 95744 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 6 2 6 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1F 10.6019/CHEMBL2364335
CHEMBL2364430 95744 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 6 2 6 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1F 10.6019/CHEMBL2364335
69197228 95790 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 445 5 2 5 4.6 C[C@H]1CN(c2ccc(Cl)c(NS(=O)(=O)c3ccc(-c4ccco4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364475 95790 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 445 5 2 5 4.6 C[C@H]1CN(c2ccc(Cl)c(NS(=O)(=O)c3ccc(-c4ccco4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
16114291 198073 1 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/acs.jmedchem.1c02191
CHEMBL5190973 198073 1 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/acs.jmedchem.1c02191
16114292 103709 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm701292s
CHEMBL266063 103709 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm701292s
9875705 212080 1 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
CHEMBL79263 212080 1 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
44436850 98324 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 564 11 4 6 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL240509 98324 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 564 11 4 6 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44447840 101767 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 497 14 4 10 0.9 CC(C)(N)C(=O)N[C@H](COCc1cccc(Cl)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254766 101767 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 497 14 4 10 0.9 CC(C)(N)C(=O)N[C@H](COCc1cccc(Cl)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44447854 101740 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 469 14 4 10 0.7 CC(C)(N)C(=O)N[C@H](COCC1CCCCC1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254566 101740 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 469 14 4 10 0.7 CC(C)(N)C(=O)N[C@H](COCC1CCCCC1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL105462 215247 38 None 12 2 Rat 8.8 pEC50 = 8.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm980197u
44447844 101652 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.3 CC(C)(N)C(=O)N[C@H](COCc1cccc(C(F)(F)F)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL253965 101652 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.3 CC(C)(N)C(=O)N[C@H](COCc1cccc(C(F)(F)F)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44450017 103121 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 461 15 4 9 0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL261544 103121 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 461 15 4 9 0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCO 10.1016/j.bmcl.2008.03.059
10118326 30865 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 509 9 4 4 3.7 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1ccc2ccccc2c1)C1CCNCC1 10.1016/j.bmc.2007.01.057
CHEMBL133848 30865 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 509 9 4 4 3.7 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1ccc2ccccc2c1)C1CCNCC1 10.1016/j.bmc.2007.01.057
10458218 34260 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CC(=O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
CHEMBL13687 34260 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CC(=O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
10745618 119764 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 568 13 2 4 4.5 CN(C(=O)/C=C/CC(C)(C)N)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)NCC1CC1 10.1021/jm980197u
CHEMBL331093 119764 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 568 13 2 4 4.5 CN(C(=O)/C=C/CC(C)(C)N)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)NCC1CC1 10.1021/jm980197u
10118326 30865 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 509 9 4 4 3.7 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1ccc2ccccc2c1)C1CCNCC1 10.1016/j.bmc.2007.01.057
CHEMBL133848 30865 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 509 9 4 4 3.7 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1ccc2ccccc2c1)C1CCNCC1 10.1016/j.bmc.2007.01.057
156010457 183833 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4632657 183833 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2)on1 10.1021/acs.jmedchem.0c00828
23649669 160746 9 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL398372 160746 9 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.03.059
23649669 160746 9 None - 1 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1021/jm7010595
CHEMBL398372 160746 9 None - 1 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1021/jm7010595
23649669 160746 9 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.05.100
CHEMBL398372 160746 9 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.05.100
23649669 160746 9 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL398372 160746 9 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44437955 17097 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 534 11 4 6 2.6 NCC(O)CNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCCN1C(=O)CCSc2ccccc21 10.1016/j.bmc.2007.01.057
CHEMBL1162063 17097 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 534 11 4 6 2.6 NCC(O)CNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCCN1C(=O)CCSc2ccccc21 10.1016/j.bmc.2007.01.057
10626337 108002 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1016/j.bmc.2007.01.057
CHEMBL295984 108002 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1016/j.bmc.2007.01.057
156010457 183833 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4632657 183833 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2)on1 10.1021/acs.jmedchem.0c00828
156012445 184114 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637284 184114 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156015928 184360 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4640615 184360 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44452750 103032 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 481 7 2 6 4.4 COc1cccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)cc2)c1 10.1016/j.bmcl.2007.12.021
CHEMBL261030 103032 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 481 7 2 6 4.4 COc1cccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)cc2)c1 10.1016/j.bmcl.2007.12.021
44452932 104363 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 475 6 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1F 10.1016/j.bmcl.2007.12.021
CHEMBL270790 104363 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 475 6 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1F 10.1016/j.bmcl.2007.12.021
44570700 190738 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 486 6 2 6 2.1 COc1cccc(C(=O)Nc2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@H](N)C3)cc2)c1 10.1016/j.bmcl.2008.12.042
CHEMBL481620 190738 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 486 6 2 6 2.1 COc1cccc(C(=O)Nc2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@H](N)C3)cc2)c1 10.1016/j.bmcl.2008.12.042
69197169 95711 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364399 95711 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11641478 95719 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)s1 10.6019/CHEMBL2364335
CHEMBL2364407 95719 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)s1 10.6019/CHEMBL2364335
24803350 95755 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1C 10.6019/CHEMBL2364335
CHEMBL2364441 95755 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1C 10.6019/CHEMBL2364335
11547664 95795 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)c2)c(F)c1 10.6019/CHEMBL2364335
CHEMBL2364480 95795 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)c2)c(F)c1 10.6019/CHEMBL2364335
44579802 193547 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(Cc1cccc(Cl)c1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL488965 193547 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(Cc1cccc(Cl)c1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44444572 100794 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 498 5 1 7 4.1 COc1cc2c(cc1N1C[C@@H](C)NC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL248745 100794 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 498 5 1 7 4.1 COc1cc2c(cc1N1C[C@@H](C)NC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
145962494 168853 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160705 168853 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145951150 169555 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4171914 169555 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
44434120 96682 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 523 15 3 9 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCCNC(=O)OCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL237926 96682 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 523 15 3 9 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCCNC(=O)OCc1ccccc1 10.1016/j.bmcl.2007.07.099
9827234 12108 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 498 9 5 4 3.1 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1c[nH]c2ccccc12)C1CCNCC1 10.1016/j.bmc.2007.01.057
CHEMBL106841 12108 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 498 9 5 4 3.1 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1c[nH]c2ccccc12)C1CCNCC1 10.1016/j.bmc.2007.01.057
44411718 17078 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 467 7 2 5 3.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161825 17078 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 467 7 2 5 3.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
44437953 17096 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 522 9 3 6 1.5 NCCNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCN1C(=O)CCS(=O)(=O)c2ccccc21 10.1016/j.bmc.2007.01.057
CHEMBL1162062 17096 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 522 9 3 6 1.5 NCCNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCN1C(=O)CCS(=O)(=O)c2ccccc21 10.1016/j.bmc.2007.01.057
44293557 107865 0 None 1 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL294923 107865 0 None 1 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL540001 107865 0 None 1 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
127046473 146558 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 661 17 6 8 4.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798645 146558 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 661 17 6 8 4.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
156012203 184113 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 558 7 3 8 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1nnc(-c2ccc(F)cc2)s1 10.1021/acs.jmedchem.0c00828
CHEMBL4637255 184113 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 558 7 3 8 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1nnc(-c2ccc(F)cc2)s1 10.1021/acs.jmedchem.0c00828
156016696 184409 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641201 184409 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
11525404 102156 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
CHEMBL256808 102156 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
44571004 190825 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 431 5 1 5 2.6 CNC1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccc(C)o3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL482203 190825 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 431 5 1 5 2.6 CNC1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccc(C)o3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL105462 215247 38 None 12 2 Rat 8.0 pEC50 = 8 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/s0960-894x(97)10199-8
24969294 95655 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 460 5 3 6 3.1 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)c[nH]c3=O)cc2F)o1 10.6019/CHEMBL2364335
CHEMBL2364343 95655 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 460 5 3 6 3.1 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)c[nH]c3=O)cc2F)o1 10.6019/CHEMBL2364335
69194607 95670 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 466 6 2 6 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)cc1 10.6019/CHEMBL2364335
CHEMBL2364358 95670 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 466 6 2 6 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)cc1 10.6019/CHEMBL2364335
69197049 95671 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 472 6 2 7 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)s1 10.6019/CHEMBL2364335
CHEMBL2364359 95671 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 472 6 2 7 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)s1 10.6019/CHEMBL2364335
69195141 95689 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 431 5 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1csc2ccccc12 10.6019/CHEMBL2364335
CHEMBL2364377 95689 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 431 5 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1csc2ccccc12 10.6019/CHEMBL2364335
11682686 95702 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 395 4 2 4 3.8 C[C@H]1CN(c2cccc(NS(=O)(=O)c3cccc4ccccc34)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364390 95702 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 395 4 2 4 3.8 C[C@H]1CN(c2cccc(NS(=O)(=O)c3cccc4ccccc34)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69198021 95745 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc2cccc(Cl)c12 10.6019/CHEMBL2364335
CHEMBL2364431 95745 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc2cccc(Cl)c12 10.6019/CHEMBL2364335
11655608 95758 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 5 4.7 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)c(F)c3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364444 95758 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 5 4.7 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)c(F)c3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69194649 95792 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 479 5 2 5 5.2 C[C@H]1CN(c2ccc(Cl)c(NS(=O)(=O)c3ccc(-c4ccccc4F)s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364477 95792 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 479 5 2 5 5.2 C[C@H]1CN(c2ccc(Cl)c(NS(=O)(=O)c3ccc(-c4ccccc4F)s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69196750 95794 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 472 6 2 7 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)nc1 10.6019/CHEMBL2364335
CHEMBL2364479 95794 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 472 6 2 7 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)nc1 10.6019/CHEMBL2364335
23730339 154898 0 None - 1 Human 8.0 pEC50 = 8 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 475 10 3 10 0.4 CC1(O)CCN(C(=O)OCCn2nnnc2[C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)C1 10.1021/jm7010595
CHEMBL393531 154898 0 None - 1 Human 8.0 pEC50 = 8 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 475 10 3 10 0.4 CC1(O)CCN(C(=O)OCCn2nnnc2[C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)C1 10.1021/jm7010595
156016696 184409 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641201 184409 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145993528 174097 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 561 5 1 4 6.6 C#Cc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4294083 174097 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 561 5 1 4 6.6 C#Cc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
156012203 184113 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 558 7 3 8 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1nnc(-c2ccc(F)cc2)s1 10.1021/acs.jmedchem.0c00828
CHEMBL4637255 184113 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 558 7 3 8 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1nnc(-c2ccc(F)cc2)s1 10.1021/acs.jmedchem.0c00828
145950201 169721 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174476 169721 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
44281466 176161 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 436 8 2 4 2.9 Cc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
CHEMBL442151 176161 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 436 8 2 4 2.9 Cc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
44452806 103458 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 486 7 2 7 4.6 CC(C)Oc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
CHEMBL263916 103458 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 486 7 2 7 4.6 CC(C)Oc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
44452885 104590 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 481 8 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL271948 104590 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 481 8 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2007.12.021
11633712 166114 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 446 5 2 6 3.9 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
CHEMBL410013 166114 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 446 5 2 6 3.9 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
57390496 75830 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
CHEMBL1923628 75830 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
56926782 75832 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 472 4 3 4 3.0 CC[C@H](C)[C@@H]1NCCCCCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923631 75832 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 472 4 3 4 3.0 CC[C@H](C)[C@@H]1NCCCCCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926785 75835 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923634 75835 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926892 75837 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923636 75837 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926893 75838 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 nan
CHEMBL1923637 75838 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 nan
134131183 149246 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3890296 149246 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134133488 150014 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 600 4 4 5 4.1 CC[C@H](C)[C@@H]1NCCOc2ccc(F)cc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3896536 150014 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 600 4 4 5 4.1 CC[C@H](C)[C@@H]1NCCOc2ccc(F)cc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134134870 151170 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 534 3 4 5 2.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3905987 151170 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 534 3 4 5 2.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134132958 151439 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 536 3 3 5 2.4 C[C@H]1C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)NC[C@H]2C[C@@H]2c2ccccc2OCCN[C@H](C2CC2)C(=O)N1C nan
CHEMBL3908264 151439 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 536 3 3 5 2.4 C[C@H]1C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)NC[C@H]2C[C@@H]2c2ccccc2OCCN[C@H](C2CC2)C(=O)N1C nan
134132265 151749 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 548 3 4 6 2.2 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOCC2)NC1=O nan
CHEMBL3910661 151749 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 548 3 4 6 2.2 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOCC2)NC1=O nan
76460236 152238 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 472 4 3 4 3.0 CCC(C)C1NCCCCCCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3914338 152238 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 472 4 3 4 3.0 CCC(C)C1NCCCCCCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
134141159 153507 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 523 4 3 6 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3924192 153507 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 523 4 3 6 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](C)N(C)C1=O nan
134149092 155232 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 4 4 5 2.5 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O nan
CHEMBL3937924 155232 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 4 4 5 2.5 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O nan
134146570 155559 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3940653 155559 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134145820 155813 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 4 2.9 CC[C@H](C)[C@@H]1NCCc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3942642 155813 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 4 2.9 CC[C@H](C)[C@@H]1NCCc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134155024 157791 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 4 3 4 3.6 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3958451 157791 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 4 3 4 3.6 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134155282 158121 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3961108 158121 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134152627 158327 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 504 4 3 4 3.0 CC[C@H](C)[C@@H]1NCc2ccccc2C/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3963078 158327 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 504 4 3 4 3.0 CC[C@H](C)[C@@H]1NCc2ccccc2C/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134150696 158858 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 4 3.2 CCC(C)C1NCc2ccccc2CCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3967506 158858 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 4 3.2 CCC(C)C1NCc2ccccc2CCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
134150029 158894 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 518 4 3 4 3.3 CC[C@H](C)C1NCCCc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3967783 158894 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 518 4 3 4 3.3 CC[C@H](C)C1NCCCc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
134153608 159149 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 4 3.2 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3970180 159149 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 4 3.2 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134154022 159604 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 532 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3973940 159604 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 532 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134151899 160098 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3978207 160098 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
134156625 160430 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 472 4 3 5 1.7 CC[C@H](C)[C@@H]1NCCOC/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3981072 160430 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 472 4 3 5 1.7 CC[C@H](C)[C@@H]1NCCOC/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
16040587 186163 0 None -14 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human Ghrelin receptorAgonist activity at human Ghrelin receptor
ChEMBL 501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1 10.1021/jm801332q
CHEMBL473921 186163 0 None -14 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human Ghrelin receptorAgonist activity at human Ghrelin receptor
ChEMBL 501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1 10.1021/jm801332q
44576247 221001 0 None - 1 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.1c02191
CHEMBL506986 221001 0 None - 1 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.1c02191
44576247 221001 0 None - 1 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayInverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1016/j.bmcl.2016.04.003
CHEMBL506986 221001 0 None - 1 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayInverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1016/j.bmcl.2016.04.003
CHEMBL3578015 218545 0 None -33 2 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
CHEMBL3578018 218548 0 None -15 2 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
69198097 95676 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 452 6 2 6 3.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccnc2)cc1 10.6019/CHEMBL2364335
CHEMBL2364364 95676 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 452 6 2 6 3.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccnc2)cc1 10.6019/CHEMBL2364335
69198438 95678 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccnc2)s1 10.6019/CHEMBL2364335
CHEMBL2364366 95678 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccnc2)s1 10.6019/CHEMBL2364335
69196473 95687 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 452 5 2 6 4.3 C[C@H]1CN(c2cc(NS(=O)(=O)c3ccc(-c4cccs4)cc3)ccc2C#N)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364375 95687 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 452 5 2 6 4.3 C[C@H]1CN(c2cc(NS(=O)(=O)c3ccc(-c4cccs4)cc3)ccc2C#N)C[C@@H](C)N1 10.6019/CHEMBL2364335
69197657 95688 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 497 8 2 7 4.5 COc1ccc(Oc2cccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)c2)cc1 10.6019/CHEMBL2364335
CHEMBL2364376 95688 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 497 8 2 7 4.5 COc1ccc(Oc2cccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)c2)cc1 10.6019/CHEMBL2364335
69195983 95709 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 6 2 5 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccc3C)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364397 95709 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 6 2 5 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccc3C)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69196844 95726 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(F)cc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364414 95726 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(F)cc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11647817 95730 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 437 4 2 4 3.7 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)cc1 10.6019/CHEMBL2364335
CHEMBL2364418 95730 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 437 4 2 4 3.7 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)cc1 10.6019/CHEMBL2364335
69196864 95748 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 487 6 2 5 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(F)cc2F)cc1 10.6019/CHEMBL2364335
CHEMBL2364434 95748 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 487 6 2 5 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(F)cc2F)cc1 10.6019/CHEMBL2364335
69198407 95777 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 5 2 5 3.6 COc1cc(Br)ccc1S(=O)(=O)Nc1cc(N2C[C@H](C)N[C@H](C)C2)ccc1F 10.6019/CHEMBL2364335
CHEMBL2364463 95777 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 5 2 5 3.6 COc1cc(Br)ccc1S(=O)(=O)Nc1cc(N2C[C@H](C)N[C@H](C)C2)ccc1F 10.6019/CHEMBL2364335
44579958 198121 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 381 7 2 4 3.2 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
CHEMBL519171 198121 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 381 7 2 4 3.2 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
156020713 184867 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 477 6 3 7 0.7 Cc1csc(C(=O)N[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2C(=O)N[C@H]2CCCNC2)n1 10.1021/acs.jmedchem.0c00828
CHEMBL4647751 184867 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 477 6 3 7 0.7 Cc1csc(C(=O)N[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2C(=O)N[C@H]2CCCNC2)n1 10.1021/acs.jmedchem.0c00828
134139753 152814 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 5 3 5 2.5 CCCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3918783 152814 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 5 3 5 2.5 CCCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
44449923 103113 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 601 17 4 11 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1cccc(S(=O)(=O)CCO)c1 10.1016/j.bmcl.2008.03.059
CHEMBL261497 103113 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 601 17 4 11 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1cccc(S(=O)(=O)CCO)c1 10.1016/j.bmcl.2008.03.059
156020713 184867 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 477 6 3 7 0.7 Cc1csc(C(=O)N[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2C(=O)N[C@H]2CCCNC2)n1 10.1021/acs.jmedchem.0c00828
CHEMBL4647751 184867 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 477 6 3 7 0.7 Cc1csc(C(=O)N[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2C(=O)N[C@H]2CCCNC2)n1 10.1021/acs.jmedchem.0c00828
44434110 95287 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 515 13 3 9 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL235135 95287 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 515 13 3 9 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL3578018 218548 0 None -15 2 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
44450102 102546 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 511 14 4 10 0.6 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1ccccc1C(=O)NCCO 10.1016/j.bmcl.2008.03.059
CHEMBL258550 102546 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 511 14 4 10 0.6 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1ccccc1C(=O)NCCO 10.1016/j.bmcl.2008.03.059
16114290 143986 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 534 11 3 5 5.3 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL374992 143986 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 534 11 3 5 5.3 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
11664206 75828 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923626 75828 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
71453489 216147 15 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Val mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Val mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 216147 15 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Val mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Val mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
9870965 71088 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 509 9 1 5 5.3 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181092 71088 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 509 9 1 5 5.3 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44434051 96190 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccccc2)n1 10.1016/j.bmcl.2007.07.099
CHEMBL237058 96190 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccccc2)n1 10.1016/j.bmcl.2007.07.099
44434053 153636 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1cccc(NS(C)(=O)=O)c1 10.1016/j.bmcl.2007.07.099
CHEMBL392522 153636 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1cccc(NS(C)(=O)=O)c1 10.1016/j.bmcl.2007.07.099
145988557 174039 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 523 4 1 2 6.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C#CC3CC3)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4292914 174039 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 523 4 1 2 6.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C#CC3CC3)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL2170775 216142 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44434083 96806 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 420 10 2 7 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C/C=C/c1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL238155 96806 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 420 10 2 7 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C/C=C/c1ccccc1 10.1016/j.bmcl.2007.07.099
44436884 98327 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 565 11 5 7 3.1 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL240522 98327 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 565 11 5 7 3.1 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
16114098 148389 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 534 11 3 5 5.4 Cc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL385131 148389 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 534 11 3 5 5.4 Cc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
16113246 101452 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252643 101452 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
22888486 71092 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 552 9 2 6 5.5 CC(=O)Nc1cccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)c1 10.1016/j.bmcl.2005.02.040
CHEMBL181108 71092 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 552 9 2 6 5.5 CC(=O)Nc1cccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)c1 10.1016/j.bmcl.2005.02.040
71453489 216147 15 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02122
CHEMBL2170781 216147 15 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02122
156018539 184588 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1NC(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4643595 184588 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1NC(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
145949755 169713 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174302 169713 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
156013970 184019 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 624 7 3 6 3.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1ccc(-c2cc(C(F)(F)F)ccc2Cl)o1 10.1021/acs.jmedchem.0c00828
CHEMBL4635743 184019 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 624 7 3 6 3.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1ccc(-c2cc(C(F)(F)F)ccc2Cl)o1 10.1021/acs.jmedchem.0c00828
156018539 184588 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1NC(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4643595 184588 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1NC(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
69197178 95648 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(Cl)s2)cc1 10.6019/CHEMBL2364335
CHEMBL2364336 95648 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(Cl)s2)cc1 10.6019/CHEMBL2364335
69194396 95699 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 7 2 6 4.8 CCOc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364387 95699 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 7 2 6 4.8 CCOc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
69195258 95731 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 447 6 2 7 4.0 COc1ccc(NS(=O)(=O)c2ccc(-c3ccoc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364419 95731 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 447 6 2 7 4.0 COc1ccc(NS(=O)(=O)c2ccc(-c3ccoc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11604627 95747 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1ccc(NS(=O)(=O)c2ccc(-c3ccoc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364433 95747 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1ccc(NS(=O)(=O)c2ccc(-c3ccoc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69197381 95765 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 486 6 2 7 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc(C)c(-c2cccc(C)n2)s1 10.6019/CHEMBL2364335
CHEMBL2364451 95765 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 486 6 2 7 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc(C)c(-c2cccc(C)n2)s1 10.6019/CHEMBL2364335
11576185 95772 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2nccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364458 95772 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2nccs2)cc1 10.6019/CHEMBL2364335
11633856 95798 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 453 6 2 7 3.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ncccn2)cc1 10.6019/CHEMBL2364335
CHEMBL2364483 95798 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 453 6 2 7 3.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ncccn2)cc1 10.6019/CHEMBL2364335
59007104 95801 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 1 6 4.8 COc1ccc(N2C[C@H](C)N(C)[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364486 95801 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 1 6 4.8 COc1ccc(N2C[C@H](C)N(C)[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2170779 216145 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44579824 190889 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1cccc(CN(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)c1 10.1016/j.bmcl.2008.07.120
CHEMBL482623 190889 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1cccc(CN(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)c1 10.1016/j.bmcl.2008.07.120
44579883 193616 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL489403 193616 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.120
44579861 200979 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1ccccc1 10.1016/j.bmcl.2008.07.120
CHEMBL528332 200979 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1ccccc1 10.1016/j.bmcl.2008.07.120
44579906 199398 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)[C@@H](C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL521612 199398 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)[C@@H](C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
145992125 173529 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 552 5 2 5 6.2 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(N)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4283504 173529 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 552 5 2 5 6.2 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(N)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
156016682 184545 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4642860 184545 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL2170776 216143 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(C(C)(C)C)cc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
16752689 195147 0 None -5 3 Rabbit 6.9 pEC50 = 6.9 Functional
Activity at ghrelin receptor in New Zealand White rabbit gastric antral smooth muscle by calcium mobilization-based FLIPR assayActivity at ghrelin receptor in New Zealand White rabbit gastric antral smooth muscle by calcium mobilization-based FLIPR assay
ChEMBL 568 10 2 4 6.6 COc1cccc(CCN(Cc2ccccc2-c2ccc(CN3C[C@H](C)N[C@H](C)C3)cc2)C(=O)NC2CCCCC2)c1 10.1016/j.bmcl.2008.10.071
CHEMBL501315 195147 0 None -5 3 Rabbit 6.9 pEC50 = 6.9 Functional
Activity at ghrelin receptor in New Zealand White rabbit gastric antral smooth muscle by calcium mobilization-based FLIPR assayActivity at ghrelin receptor in New Zealand White rabbit gastric antral smooth muscle by calcium mobilization-based FLIPR assay
ChEMBL 568 10 2 4 6.6 COc1cccc(CCN(Cc2ccccc2-c2ccc(CN3C[C@H](C)N[C@H](C)C3)cc2)C(=O)NC2CCCCC2)c1 10.1016/j.bmcl.2008.10.071
44444557 161465 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 493 4 0 5 3.7 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(S(=O)(=O)c1cccc(Br)c1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL399704 161465 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 493 4 0 5 3.7 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(S(=O)(=O)c1cccc(Br)c1)CC2 10.1016/j.bmcl.2007.09.067
145957404 168828 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)c(F)cc21 10.1021/acs.jmedchem.8b00322
CHEMBL4160261 168828 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)c(F)cc21 10.1021/acs.jmedchem.8b00322
145955250 169303 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 4 4 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCOC3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4167776 169303 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 4 4 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCOC3)cc2c1 10.1021/acs.jmedchem.8b00322
145950261 169508 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4171137 169508 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
156014569 184011 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 599 7 2 7 2.5 CC(=O)N1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
CHEMBL4635694 184011 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 599 7 2 7 2.5 CC(=O)N1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
44452776 103103 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 453 5 2 5 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL261466 103103 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 453 5 2 5 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)cc1 10.1016/j.bmcl.2007.12.021
69196695 95661 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 467 7 2 6 4.5 COc1ccc(NS(=O)(=O)c2ccc(Oc3ccccc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364349 95661 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 467 7 2 6 4.5 COc1ccc(NS(=O)(=O)c2ccc(Oc3ccccc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
59007058 95669 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 6 3.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)s1 10.6019/CHEMBL2364335
CHEMBL2364357 95669 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 6 3.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)s1 10.6019/CHEMBL2364335
156016682 184545 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4642860 184545 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44579842 191530 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccccc1Cl 10.1016/j.bmcl.2008.07.120
CHEMBL485091 191530 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccccc1Cl 10.1016/j.bmcl.2008.07.120
145986461 173992 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4291926 173992 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
145950261 169508 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4171137 169508 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
10602593 119619 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 542 12 2 4 4.1 CCNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL330860 119619 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 542 12 2 4 4.1 CCNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
44391038 71359 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 555 13 1 4 5.9 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CCCc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181627 71359 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 555 13 1 4 5.9 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CCCc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL2170783 216149 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](NC(=O)[C@@H](N)CCCCN)C(c1ccccc1)c1ccccc1)C(N)=O 10.1021/jm300414b
CHEMBL2170779 216145 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
156013970 184019 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 624 7 3 6 3.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1ccc(-c2cc(C(F)(F)F)ccc2Cl)o1 10.1021/acs.jmedchem.0c00828
CHEMBL4635743 184019 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 624 7 3 6 3.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1ccc(-c2cc(C(F)(F)F)ccc2Cl)o1 10.1021/acs.jmedchem.0c00828
156014569 184011 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 599 7 2 7 2.5 CC(=O)N1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
CHEMBL4635694 184011 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 599 7 2 7 2.5 CC(=O)N1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
56926173 75787 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923501 75787 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
134138625 154809 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 494 3 3 5 1.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3934561 154809 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 494 3 3 5 1.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
155526063 177815 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1174 34 16 14 -2.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4456830 177815 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1174 34 16 14 -2.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
145957404 168828 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)c(F)cc21 10.1021/acs.jmedchem.8b00322
CHEMBL4160261 168828 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)c(F)cc21 10.1021/acs.jmedchem.8b00322
145955250 169303 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 4 4 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCOC3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4167776 169303 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 4 4 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCOC3)cc2c1 10.1021/acs.jmedchem.8b00322
44454060 162111 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL403180 162111 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
57399248 75819 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at ghrelin receptor by cell based assayAgonist activity at ghrelin receptor by cell based assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm1012374
CHEMBL1923617 75819 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at ghrelin receptor by cell based assayAgonist activity at ghrelin receptor by cell based assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm1012374
145949755 169713 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174302 169713 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
44434109 153059 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 529 13 2 9 1.8 CN(c1ccccc1CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N)S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL392076 153059 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 529 13 2 9 1.8 CN(c1ccccc1CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N)S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
9890375 105046 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL274599 105046 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL558802 105046 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
44436876 153797 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 580 11 4 7 4.6 COc1ccc(N2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL392663 153797 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 580 11 4 7 4.6 COc1ccc(N2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
9890375 105046 0 None -1 3 Rat 7.9 pEC50 = 7.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/s0960-894x(97)10199-8
CHEMBL274599 105046 0 None -1 3 Rat 7.9 pEC50 = 7.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/s0960-894x(97)10199-8
CHEMBL558802 105046 0 None -1 3 Rat 7.9 pEC50 = 7.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/s0960-894x(97)10199-8
9890375 105046 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL274599 105046 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL558802 105046 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
44281466 176161 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 436 8 2 4 2.9 Cc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
CHEMBL442151 176161 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 436 8 2 4 2.9 Cc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
162672839 189801 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 681 14 3 7 5.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4793824 189801 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 681 14 3 7 5.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.9b02122
22888428 71124 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 508 9 2 4 4.9 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)NC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181247 71124 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 508 9 2 4 4.9 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)NC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
23730227 154652 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 477 15 4 10 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCCO 10.1021/jm7010595
CHEMBL393330 154652 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 477 15 4 10 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCCO 10.1021/jm7010595
44450133 167172 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 481 13 3 10 -0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCNC(=O)CCS(C)(=O)=O 10.1016/j.bmcl.2008.03.059
CHEMBL411122 167172 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 481 13 3 10 -0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCNC(=O)CCS(C)(=O)=O 10.1016/j.bmcl.2008.03.059
44579821 191007 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1ccccc1Cl 10.1016/j.bmcl.2008.07.120
CHEMBL483455 191007 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1ccccc1Cl 10.1016/j.bmcl.2008.07.120
44579879 193774 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)c1 10.1016/j.bmcl.2008.07.120
CHEMBL490627 193774 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)c1 10.1016/j.bmcl.2008.07.120
44450071 103360 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 489 15 3 10 0.6 CCOC(=O)CCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
CHEMBL263141 103360 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 489 15 3 10 0.6 CCOC(=O)CCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
16113906 144001 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 612 12 5 5 6.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
CHEMBL375102 144001 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 612 12 5 5 6.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
44579752 193739 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 377 8 1 4 3.7 CCC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(CC#N)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL490390 193739 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 377 8 1 4 3.7 CCC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(CC#N)cc1 10.1016/j.bmcl.2008.07.120
44436887 97734 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 563 11 5 6 3.7 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL239464 97734 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 563 11 5 6 3.7 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44434076 96552 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 513 10 2 9 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC1CN(S(C)(=O)=O)c2ccccc21 10.1016/j.bmcl.2007.07.099
CHEMBL237717 96552 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 513 10 2 9 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC1CN(S(C)(=O)=O)c2ccccc21 10.1016/j.bmcl.2007.07.099
145952740 169280 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4167481 169280 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
23648250 85938 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 585 10 4 5 6.0 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
CHEMBL2113327 85938 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 585 10 4 5 6.0 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
16113577 91711 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 573 12 4 5 5.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
CHEMBL223725 91711 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 573 12 4 5 5.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
162657465 187820 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 652 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc[nH]2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4759418 187820 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 652 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc[nH]2)cc1 10.1021/acs.jmedchem.9b02122
44444574 100795 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 484 5 1 7 3.8 COc1cc2c(cc1N1CCNC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL248746 100795 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 484 5 1 7 3.8 COc1cc2c(cc1N1CCNC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
145952740 169280 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4167481 169280 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
11532288 103695 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 441 6 2 7 2.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-n2cccn2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL265950 103695 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 441 6 2 7 2.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-n2cccn2)cc1 10.1016/j.bmcl.2007.12.021
11576186 162004 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 458 6 2 7 3.8 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccn3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.1016/j.bmcl.2007.12.021
CHEMBL402632 162004 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 458 6 2 7 3.8 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccn3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.1016/j.bmcl.2007.12.021
44570964 190660 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 407 4 1 5 1.7 Cc1ccc(-c2ccc(S(=O)(=O)N3CC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL481014 190660 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 407 4 1 5 1.7 Cc1ccc(-c2ccc(S(=O)(=O)N3CC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
44570921 190734 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 413 4 1 4 2.5 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL481601 190734 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 413 4 1 4 2.5 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
59007073 95649 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 442 6 2 7 3.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)nc1 10.6019/CHEMBL2364335
CHEMBL2364337 95649 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 442 6 2 7 3.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)nc1 10.6019/CHEMBL2364335
69197749 95658 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 425 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2ccc3ccccc3c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364346 95658 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 425 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2ccc3ccccc3c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11682796 95660 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 401 6 2 5 3.3 COc1ccc(NS(=O)(=O)/C=C/c2ccccc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364348 95660 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 401 6 2 5 3.3 COc1ccc(NS(=O)(=O)/C=C/c2ccccc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69198460 95672 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.6019/CHEMBL2364335
CHEMBL2364360 95672 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.6019/CHEMBL2364335
69198360 95680 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 466 6 2 6 4.1 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)n3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364368 95680 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 466 6 2 6 4.1 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)n3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11683967 95692 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2cccs2)c1 10.6019/CHEMBL2364335
CHEMBL2364380 95692 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2cccs2)c1 10.6019/CHEMBL2364335
69195261 95700 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 7 2 6 5.2 CC(C)Oc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364388 95700 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 7 2 6 5.2 CC(C)Oc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
11516766 95704 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 395 4 2 4 3.8 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc4ccccc4c3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364392 95704 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 395 4 2 4 3.8 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc4ccccc4c3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11525161 95761 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 447 5 2 5 4.2 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)c(F)c3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364447 95761 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 447 5 2 5 4.2 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)c(F)c3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69194533 95791 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 6 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc(F)c(-c2ccco2)cc1F 10.6019/CHEMBL2364335
CHEMBL2364476 95791 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 6 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc(F)c(-c2ccco2)cc1F 10.6019/CHEMBL2364335
69197165 95803 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 427 5 3 6 3.6 C[C@H]1CN(c2ccc(O)c(NS(=O)(=O)c3ccc(-c4ccco4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364488 95803 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 427 5 3 6 3.6 C[C@H]1CN(c2ccc(O)c(NS(=O)(=O)c3ccc(-c4ccco4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
44579777 193763 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1)C(=O)N(Cc1ccccc1Cl)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL490601 193763 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1)C(=O)N(Cc1ccccc1Cl)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44454432 162037 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
CHEMBL402808 162037 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
44434112 175639 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2cc3ccccc3n2S(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL438154 175639 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2cc3ccccc3n2S(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
44579908 193653 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 C[C@@H](Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL489610 193653 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 C[C@@H](Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
145954311 169265 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4167267 169265 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
44434124 95433 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 343 8 2 8 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CC#N)n1 10.1016/j.bmcl.2007.07.099
CHEMBL235817 95433 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 343 8 2 8 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CC#N)n1 10.1016/j.bmcl.2007.07.099
162659161 188170 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 642 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)Cc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4763471 188170 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 642 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)Cc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
44444556 101177 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 471 6 0 5 4.4 CCOc1ccc(CC(=O)N2CCc3cc(OC)c(N4C[C@H](C)N(C)[C@H](C)C4)cc32)cc1Cl 10.1016/j.bmcl.2007.09.067
CHEMBL250973 101177 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 471 6 0 5 4.4 CCOc1ccc(CC(=O)N2CCc3cc(OC)c(N4C[C@H](C)N(C)[C@H](C)C4)cc32)cc1Cl 10.1016/j.bmcl.2007.09.067
145950963 169585 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4172411 169585 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145952396 169782 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
CHEMBL4175534 169782 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
156011695 184134 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 8 2 7 2.2 O=CN1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
CHEMBL4637585 184134 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 8 2 7 2.2 O=CN1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
44452887 166357 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 451 6 2 5 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2007.12.021
CHEMBL410282 166357 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 451 6 2 5 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2007.12.021
46882522 12484 0 None -39 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 440 7 2 5 3.6 CC(C)Oc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1078208 12484 0 None -39 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 440 7 2 5 3.6 CC(C)Oc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
69195349 95683 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 453 5 2 5 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(Br)c1 10.6019/CHEMBL2364335
CHEMBL2364371 95683 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 453 5 2 5 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(Br)c1 10.6019/CHEMBL2364335
69198352 95804 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 6 2 6 4.0 COc1ccc(N2CCN[C@@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364489 95804 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 6 2 6 4.0 COc1ccc(N2CCN[C@@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
44446188 162170 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL403542 162170 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
145954311 169265 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4167267 169265 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
46882521 12483 0 None -158 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 458 6 2 4 4.5 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1078207 12483 0 None -158 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 458 6 2 4 4.5 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.09.027
44445620 161457 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 571 11 2 6 6.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccc2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL399651 161457 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 571 11 2 6 6.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccc2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
22862453 105235 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 490 5 4 5 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CC(O)c1ccccc1O2 10.1016/s0960-894x(97)10199-8
CHEMBL275795 105235 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 490 5 4 5 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CC(O)c1ccccc1O2 10.1016/s0960-894x(97)10199-8
10675061 103318 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 598 13 2 5 4.3 CN(C(=O)/C=C/CC(C)(C)N)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)NCC1CCCO1 10.1021/jm980197u
CHEMBL262889 103318 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 598 13 2 5 4.3 CN(C(=O)/C=C/CC(C)(C)N)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)NCC1CCCO1 10.1021/jm980197u
10026738 169548 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL417182 169548 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL557206 169548 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
56926464 75814 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)N(C)C1=O nan
CHEMBL1923612 75814 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)N(C)C1=O nan
155540883 179736 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.36 +/- 0.01 nM)Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.36 +/- 0.01 nM)
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4517399 179736 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.36 +/- 0.01 nM)Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.36 +/- 0.01 nM)
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
10210658 17098 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 593 13 5 5 3.6 NCCCCNC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1 10.1016/j.bmc.2007.01.057
CHEMBL1162064 17098 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 593 13 5 5 3.6 NCCCCNC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1 10.1016/j.bmc.2007.01.057
145952396 169782 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
CHEMBL4175534 169782 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
CHEMBL2170784 216150 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
134139080 154461 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 4 4 5 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
CHEMBL3931856 154461 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 4 4 5 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
156011695 184134 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 8 2 7 2.2 O=CN1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
CHEMBL4637585 184134 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 8 2 7 2.2 O=CN1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
CHEMBL2170697 216136 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44434080 96686 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2007.07.099
44434080 96686 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL237933 96686 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL237933 96686 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2008.01.100
10210658 17098 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 593 13 5 5 3.6 NCCCCNC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1 10.1016/j.bmc.2007.01.057
CHEMBL1162064 17098 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 593 13 5 5 3.6 NCCCCNC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1 10.1016/j.bmc.2007.01.057
10026738 169548 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL417182 169548 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL557206 169548 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
10530983 175164 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 564 11 2 4 4.0 CNC(=O)[C@@H](Cc1ccc(F)c(F)c1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL434609 175164 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 564 11 2 4 4.0 CNC(=O)[C@@H](Cc1ccc(F)c(F)c1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
44391003 130099 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 531 10 1 4 5.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)c1ccccc1F)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL361612 130099 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 531 10 1 4 5.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)c1ccccc1F)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL2170780 216146 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
145950963 169585 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4172411 169585 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
127047409 146409 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 888 24 8 10 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C(CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797639 146409 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 888 24 8 10 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C(CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
10745533 146898 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL380096 146898 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
44437971 209299 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 7 2 4 3.9 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
CHEMBL611489 209299 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 7 2 4 3.9 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
16113693 144794 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 589 12 4 6 5.6 COc1cccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL376471 144794 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 589 12 4 6 5.6 COc1cccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
11692516 75823 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 554 3 3 5 3.1 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923621 75823 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 554 3 3 5 3.1 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
155557019 181366 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.34 +/- 0.12 nM)Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.34 +/- 0.12 nM)
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4556887 181366 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.34 +/- 0.12 nM)Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.34 +/- 0.12 nM)
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
9810101 106025 17 None -5 2 Rat 7.8 pEC50 = 7.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL281764 106025 17 None -5 2 Rat 7.8 pEC50 = 7.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
10745533 146898 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL380096 146898 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
44437971 209299 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 7 2 4 3.9 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
CHEMBL611489 209299 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 7 2 4 3.9 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
44579909 193682 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL489819 193682 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
44436882 152794 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 524 10 4 6 4.2 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1Cc1ccco1)C1CCNCC1 10.1021/jm0704550
CHEMBL391859 152794 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 524 10 4 6 4.2 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1Cc1ccco1)C1CCNCC1 10.1021/jm0704550
CHEMBL2170698 216137 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44434122 96286 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 385 11 2 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCCCC#N)n1 10.1016/j.bmcl.2007.07.099
CHEMBL237302 96286 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 385 11 2 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCCCC#N)n1 10.1016/j.bmcl.2007.07.099
145992142 173550 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 475 4 2 3 5.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(O)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4283858 173550 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 475 4 2 3 5.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(O)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL3578006 218539 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)O 10.1021/jm501702q
145953016 169366 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
CHEMBL4168863 169366 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
44454304 104379 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
CHEMBL270876 104379 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
44454092 104425 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
CHEMBL271082 104425 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
44454338 104611 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL272085 104611 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
22867310 36814 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 474 5 4 4 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)Cc1ccccc1C2O 10.1016/s0960-894x(97)10199-8
CHEMBL13891 36814 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 474 5 4 4 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)Cc1ccccc1C2O 10.1016/s0960-894x(97)10199-8
162653802 187310 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 656 15 4 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CCc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4753592 187310 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 656 15 4 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CCc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
44436886 168734 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 595 12 5 8 3.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL415674 168734 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 595 12 5 8 3.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
9987037 18804 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1183385 18804 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL294324 18804 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
44391008 71641 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 481 9 1 5 4.6 CCN(CC)CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL182137 71641 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 481 9 1 5 4.6 CCN(CC)CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
22888379 175092 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 584 12 2 5 4.8 CC(=O)NC(C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C)c1ccccc1 10.1016/j.bmcl.2005.02.040
CHEMBL434152 175092 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 584 12 2 5 4.8 CC(=O)NC(C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C)c1ccccc1 10.1016/j.bmcl.2005.02.040
44444564 101247 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 478 5 1 6 3.7 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1cccc(-c3ccccn3)c1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL251366 101247 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 478 5 1 6 3.7 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1cccc(-c3ccccn3)c1)CC2 10.1016/j.bmcl.2007.09.067
145961213 168942 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 3 4 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@H]3COCCN(C)C3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4162174 168942 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 3 4 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@H]3COCCN(C)C3)cc2c1 10.1021/acs.jmedchem.8b00322
145953016 169366 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
CHEMBL4168863 169366 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
145949595 169503 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4171040 169503 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145974293 169803 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4175823 169803 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
44452929 104319 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2ccco2)c1 10.1016/j.bmcl.2007.12.021
CHEMBL270573 104319 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2ccco2)c1 10.1016/j.bmcl.2007.12.021
46882396 12616 0 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 452 8 2 4 4.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cnc(C)[nH]2)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1079187 12616 0 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 452 8 2 4 4.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cnc(C)[nH]2)CC3)cc1 10.1016/j.bmcl.2009.09.027
44570698 190737 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 456 5 2 5 2.0 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(NC(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL481619 190737 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 456 5 2 5 2.0 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(NC(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
24969292 95652 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 444 5 2 6 3.8 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccn3)cc2F)o1 10.6019/CHEMBL2364335
CHEMBL2364340 95652 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 444 5 2 6 3.8 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccn3)cc2F)o1 10.6019/CHEMBL2364335
69194665 95685 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 476 6 2 7 3.9 COc1cc(F)c(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.6019/CHEMBL2364335
CHEMBL2364373 95685 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 476 6 2 7 3.9 COc1cc(F)c(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.6019/CHEMBL2364335
11524465 95705 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 413 4 2 4 4.0 C[C@H]1CN(c2cccc(NS(=O)(=O)c3cccc(Cl)c3Cl)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364393 95705 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 413 4 2 4 4.0 C[C@H]1CN(c2cccc(NS(=O)(=O)c3cccc(Cl)c3Cl)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11576404 95716 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 469 6 2 5 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364404 95716 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 469 6 2 5 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69194865 95735 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 409 4 2 4 4.1 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc2ccccc12 10.6019/CHEMBL2364335
CHEMBL2364422 95735 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 409 4 2 4 4.1 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc2ccccc12 10.6019/CHEMBL2364335
11712498 95749 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 469 6 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2F)cc1 10.6019/CHEMBL2364335
CHEMBL2364435 95749 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 469 6 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2F)cc1 10.6019/CHEMBL2364335
69195296 95754 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 5 4.7 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)cc3F)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364440 95754 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 5 4.7 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)cc3F)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11518242 95757 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.9 Cc1cc(-c2cccs2)ccc1S(=O)(=O)Nc1cc(N2C[C@H](C)N[C@H](C)C2)ccc1F 10.6019/CHEMBL2364335
CHEMBL2364443 95757 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.9 Cc1cc(-c2cccs2)ccc1S(=O)(=O)Nc1cc(N2C[C@H](C)N[C@H](C)C2)ccc1F 10.6019/CHEMBL2364335
69197366 95762 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 5 4.7 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)cc3Cl)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364448 95762 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 5 4.7 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)cc3Cl)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11503413 95779 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 454 6 2 6 3.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccn2C)cc1 10.6019/CHEMBL2364335
CHEMBL2364465 95779 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 454 6 2 6 3.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccn2C)cc1 10.6019/CHEMBL2364335
11647900 95785 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1cc(-c2ccco2)ccc1S(=O)(=O)Nc1cccc(N2C[C@H](C)N[C@H](C)C2)c1 10.6019/CHEMBL2364335
CHEMBL2364470 95785 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1cc(-c2ccco2)ccc1S(=O)(=O)Nc1cccc(N2C[C@H](C)N[C@H](C)C2)c1 10.6019/CHEMBL2364335
11669734 95786 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1cc(-c2cccs2)ccc1S(=O)(=O)Nc1cccc(N2C[C@H](C)N[C@H](C)C2)c1 10.6019/CHEMBL2364335
CHEMBL2364471 95786 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1cc(-c2cccs2)ccc1S(=O)(=O)Nc1cccc(N2C[C@H](C)N[C@H](C)C2)c1 10.6019/CHEMBL2364335
44391007 71640 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 480 9 1 4 4.1 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)N(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL182136 71640 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 480 9 1 4 4.1 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)N(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
145994050 174124 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 615 6 1 6 7.1 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4294493 174124 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 615 6 1 6 7.1 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
156016392 184425 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641386 184425 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL3578006 218539 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)O 10.1021/jm501702q
25098836 198237 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL519322 198237 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
145957574 169080 0 None 57 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164328 169080 0 None 57 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
44411745 17080 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161827 17080 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
10626337 108002 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1016/j.bmc.2007.01.057
CHEMBL295984 108002 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1016/j.bmc.2007.01.057
156013219 184268 0 None 60 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639379 184268 0 None 60 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
22888352 70711 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 537 11 1 6 4.9 CC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180659 70711 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 537 11 1 6 4.9 CC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
22888352 70711 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 537 11 1 6 4.9 CC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180659 70711 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 537 11 1 6 4.9 CC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
10649999 23878 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 534 11 2 5 3.8 CNC(=O)[C@@H](Cc1cccs1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL125498 23878 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 534 11 2 5 3.8 CNC(=O)[C@@H](Cc1cccs1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
156015928 184360 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4640615 184360 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156012445 184114 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637284 184114 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44411634 17077 1 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161824 17077 1 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
44411634 17077 1 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161824 17077 1 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
44390986 71443 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 1 5 5.2 COc1ccccc1CC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181832 71443 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 1 5 5.2 COc1ccccc1CC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL2170695 216134 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1csc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
156011766 184087 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 569 6 2 7 2.2 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N1C[C@H]2CCNC[C@H]21)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4636780 184087 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 569 6 2 7 2.2 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N1C[C@H]2CCNC[C@H]21)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
44281449 120171 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 559 12 4 7 1.4 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)CC(=O)O)CC1 10.1016/j.bmc.2007.01.057
CHEMBL33182 120171 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 559 12 4 7 1.4 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)CC(=O)O)CC1 10.1016/j.bmc.2007.01.057
44281449 120171 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 559 12 4 7 1.4 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)CC(=O)O)CC1 10.1016/j.bmc.2007.01.057
CHEMBL33182 120171 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 559 12 4 7 1.4 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)CC(=O)O)CC1 10.1016/j.bmc.2007.01.057
23648249 85937 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 557 9 4 5 5.4 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1)C1CCNCC1 10.1021/jm0704550
CHEMBL2113326 85937 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 557 9 4 5 5.4 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1)C1CCNCC1 10.1021/jm0704550
10166594 71410 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 563 8 1 5 6.6 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccc(C(F)(F)F)cc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181786 71410 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 563 8 1 5 6.6 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccc(C(F)(F)F)cc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44391010 71648 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 541 9 1 6 6.3 CSc1ccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
CHEMBL182158 71648 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 541 9 1 6 6.3 CSc1ccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
23648244 98789 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
CHEMBL241775 98789 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
155557019 181366 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.40 +/- 0.05 nM)Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.40 +/- 0.05 nM)
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4556887 181366 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.40 +/- 0.05 nM)Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.40 +/- 0.05 nM)
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
44444565 101275 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 474 5 1 8 3.4 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccon3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL251573 101275 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 474 5 1 8 3.4 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccon3)s1)CC2 10.1016/j.bmcl.2007.09.067
145957075 169058 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164040 169058 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
44411745 17080 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161827 17080 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
156013684 184044 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccc(Cl)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4636178 184044 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccc(Cl)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
156011766 184087 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 569 6 2 7 2.2 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N1C[C@H]2CCNC[C@H]21)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4636780 184087 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 569 6 2 7 2.2 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N1C[C@H]2CCNC[C@H]21)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
11539642 104704 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 448 6 2 8 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnco2)s1 10.1016/j.bmcl.2007.12.021
CHEMBL272540 104704 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 448 6 2 8 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnco2)s1 10.1016/j.bmcl.2007.12.021
44570702 190615 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 463 4 1 5 3.1 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3C[C@H](C)N[C@H](C)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL480639 190615 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 463 4 1 5 3.1 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3C[C@H](C)N[C@H](C)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
11683968 95691 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3ccsc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364379 95691 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3ccsc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69197883 95714 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2F)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364402 95714 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2F)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69195597 95727 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2Cl)s1 10.6019/CHEMBL2364335
CHEMBL2364415 95727 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2Cl)s1 10.6019/CHEMBL2364335
59007081 95741 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 5 5.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(Cl)c2)cc1 10.6019/CHEMBL2364335
CHEMBL2364428 95741 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 5 5.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(Cl)c2)cc1 10.6019/CHEMBL2364335
11648834 95796 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)c2)cc1F 10.6019/CHEMBL2364335
CHEMBL2364481 95796 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)c2)cc1F 10.6019/CHEMBL2364335
44411753 17082 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161829 17082 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
44411753 17082 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161829 17082 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
10415000 174846 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 11 3 6 2.7 CC(C)S(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
CHEMBL432461 174846 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 11 3 6 2.7 CC(C)S(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
71453489 216147 15 None - 1 Human 8.6 pEC50 = 8.6 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Phe119:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Phe119:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 216147 15 None - 1 Human 8.6 pEC50 = 8.6 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Phe119:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Phe119:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
156013684 184044 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccc(Cl)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4636178 184044 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccc(Cl)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
10415000 174846 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 11 3 6 2.7 CC(C)S(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
CHEMBL432461 174846 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 11 3 6 2.7 CC(C)S(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
156019457 184721 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645625 184721 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44449922 102996 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 615 17 3 11 1.0 CN(CCc1cccc(S(=O)(=O)CCO)c1)C(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
CHEMBL260849 102996 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 615 17 3 11 1.0 CN(CCc1cccc(S(=O)(=O)CCO)c1)C(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
44269019 105002 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 474 5 3 4 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CCc3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
CHEMBL274340 105002 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 474 5 3 4 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CCc3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
44579840 191528 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1cccc(Cl)c1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL485090 191528 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1cccc(Cl)c1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44579907 193827 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)[C@H](C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL491044 193827 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)[C@H](C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
44579805 193845 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1Cl)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL491221 193845 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1Cl)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44434113 95424 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 452 10 2 9 1.5 COC(=O)C(c1ccccc1)n1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL235793 95424 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 452 10 2 9 1.5 COC(=O)C(c1ccccc1)n1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
127048060 146639 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 789 20 6 10 5.4 COC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799222 146639 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 789 20 6 10 5.4 COC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
57399248 75819 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923617 75819 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
44268965 30834 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 472 5 3 4 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(Cc3ccccc3C2=O)C1 10.1016/s0960-894x(97)10199-8
CHEMBL13383 30834 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 472 5 3 4 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(Cc3ccccc3C2=O)C1 10.1016/s0960-894x(97)10199-8
10675800 120571 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 654 11 2 4 4.3 CNC(=O)[C@@H](Cc1ccc(I)cc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL332414 120571 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 654 11 2 4 4.3 CNC(=O)[C@@H](Cc1ccc(I)cc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
44391002 130688 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 507 10 1 4 5.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL362798 130688 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 507 10 1 4 5.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44579857 193703 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL490009 193703 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2Cl)c1 10.1016/j.bmcl.2008.07.120
44434018 95267 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 399 8 3 8 0.9 COC(=O)CCn1nnnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL235012 95267 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 399 8 3 8 0.9 COC(=O)CCn1nnnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
44579641 193676 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 370 7 1 4 4.0 CSc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
CHEMBL489794 193676 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 370 7 1 4 4.0 CSc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
44579996 193915 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 367 7 2 4 2.8 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)COc2ccccc2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL491835 193915 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 367 7 2 4 2.8 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)COc2ccccc2)cc1 10.1016/j.bmcl.2008.07.120
44579919 198128 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 444 9 1 4 5.3 CCC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1cccc(-c2ccccc2)c1OC 10.1016/j.bmcl.2008.07.120
CHEMBL519196 198128 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 444 9 1 4 5.3 CCC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1cccc(-c2ccccc2)c1OC 10.1016/j.bmcl.2008.07.120
44454092 104425 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
CHEMBL271082 104425 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
44450070 165430 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 461 14 4 9 0.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCC(=O)O 10.1016/j.bmcl.2008.03.059
CHEMBL409258 165430 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 461 14 4 9 0.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCC(=O)O 10.1016/j.bmcl.2008.03.059
156016392 184425 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641386 184425 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145961213 168942 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 3 4 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@H]3COCCN(C)C3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4162174 168942 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 3 4 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@H]3COCCN(C)C3)cc2c1 10.1021/acs.jmedchem.8b00322
145949595 169503 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4171040 169503 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145974293 169803 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4175823 169803 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
44390905 71231 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 544 10 1 6 3.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)S(=O)(=O)N(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181337 71231 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 544 10 1 6 3.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)S(=O)(=O)N(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44391040 71235 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 577 10 1 6 5.0 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)S(=O)(=O)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181352 71235 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 577 10 1 6 5.0 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)S(=O)(=O)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
10579444 121020 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 598 13 2 5 4.3 CN(C(=O)/C=C/CC(C)(C)N)[C@H](Cc1cccc2ccccc12)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)NCC1CCCO1 10.1021/jm980197u
CHEMBL332987 121020 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 598 13 2 5 4.3 CN(C(=O)/C=C/CC(C)(C)N)[C@H](Cc1cccc2ccccc12)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)NCC1CCCO1 10.1021/jm980197u
162645413 186505 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 677 14 3 7 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4744051 186505 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 677 14 3 7 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(C)cc2)cc1 10.1021/acs.jmedchem.9b02122
44293091 194965 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL49884 194965 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
16114011 144916 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 563 10 4 5 5.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(F)cc1 10.1021/jm070024h
CHEMBL376736 144916 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 563 10 4 5 5.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(F)cc1 10.1021/jm070024h
145981343 173488 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 669 6 1 6 7.6 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@H](c3ccc(-c4cnccn4)c(Cl)c3Cl)C(F)(F)F)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4282719 173488 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 669 6 1 6 7.6 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@H](c3ccc(-c4cnccn4)c(Cl)c3Cl)C(F)(F)F)CC2)ncn1 10.1021/acs.jmedchem.8b00794
44391048 69722 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 467 8 2 5 4.2 CC(C)NCCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL178502 69722 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 467 8 2 5 4.2 CC(C)NCCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
44454399 161918 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC(C#N)Cc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL402086 161918 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC(C#N)Cc1ccccc1 10.1016/j.bmcl.2008.01.100
44293091 194965 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL49884 194965 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
155540883 179736 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4517399 179736 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
44579801 193940 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1)C(=O)N(Cc1ccc(Cl)cc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL492028 193940 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1)C(=O)N(Cc1ccc(Cl)cc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
168276220 197200 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 261 6 1 1 4.2 CCCCCCCc1cc(=O)c2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.1c02191
CHEMBL5177954 197200 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 261 6 1 1 4.2 CCCCCCCc1cc(=O)c2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.1c02191
145958774 169045 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163811 169045 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145950877 169774 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4175360 169774 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
44450135 165482 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 493 14 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1ccccc1 10.1016/j.bmcl.2008.03.059
CHEMBL409327 165482 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 493 14 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1ccccc1 10.1016/j.bmcl.2008.03.059
44454302 166159 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
CHEMBL410060 166159 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
16203237 103726 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 496 10 3 6 4.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccco1 10.1021/jm070024h
CHEMBL266199 103726 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 496 10 3 6 4.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccco1 10.1021/jm070024h
56926462 75812 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923610 75812 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
162660604 187998 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 700 15 3 9 5.0 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCN3CCCCC3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4761319 187998 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 700 15 3 9 5.0 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCN3CCCCC3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
145956753 168936 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4162000 168936 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
71453489 216147 15 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 216147 15 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44446190 101331 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL251855 101331 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
44446189 162153 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL403426 162153 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
10744738 22976 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1cccc2ccccc12)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL122420 22976 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1cccc2ccccc12)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL2170699 216138 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44454432 162037 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
CHEMBL402808 162037 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
44454397 162303 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CC(C#N)Cc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
CHEMBL404227 162303 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CC(C#N)Cc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
145949381 169494 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4170865 169494 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
22862431 37258 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 474 5 3 4 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc3O2)CC1 10.1016/s0960-894x(97)10199-8
CHEMBL13930 37258 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 474 5 3 4 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc3O2)CC1 10.1016/s0960-894x(97)10199-8
162653781 187261 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 732 15 4 8 6.2 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3c[nH]c4ccccc34)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4753046 187261 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 732 15 4 8 6.2 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3c[nH]c4ccccc34)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
156013764 184050 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 7 1 7 3.0 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1N(C)C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4636229 184050 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 7 1 7 3.0 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1N(C)C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
145958317 169092 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164531 169092 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145949381 169494 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4170865 169494 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
145950877 169774 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4175360 169774 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
156013764 184050 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 7 1 7 3.0 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1N(C)C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4636229 184050 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 7 1 7 3.0 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1N(C)C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
156020452 184813 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 4 5 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@]3(C)C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4646979 184813 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 4 5 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@]3(C)C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
24969201 95656 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 476 6 2 7 4.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)nc1NS(=O)(=O)c1ccc(-c2ccoc2)cc1Cl 10.6019/CHEMBL2364335
CHEMBL2364344 95656 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 476 6 2 7 4.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)nc1NS(=O)(=O)c1ccc(-c2ccoc2)cc1Cl 10.6019/CHEMBL2364335
69197403 95681 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 5 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc2cc(Cl)ccc2s1 10.6019/CHEMBL2364335
CHEMBL2364369 95681 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 5 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc2cc(Cl)ccc2s1 10.6019/CHEMBL2364335
59007071 95695 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 444 5 3 7 3.5 C[C@H]1CN(c2ccc(O)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364383 95695 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 444 5 3 7 3.5 C[C@H]1CN(c2ccc(O)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11547135 95708 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 461 5 2 5 5.1 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-c4ccc(Cl)s4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364396 95708 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 461 5 2 5 5.1 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-c4ccc(Cl)s4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11567764 95712 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 411 5 2 6 2.9 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-n4cccn4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364400 95712 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 411 5 2 6 2.9 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-n4cccn4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11511157 95722 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2C)s1 10.6019/CHEMBL2364335
CHEMBL2364410 95722 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2C)s1 10.6019/CHEMBL2364335
11547599 95724 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 6 5.0 COc1ccc(NS(=O)(=O)c2ccc(-c3c(C)cccc3C)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364412 95724 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 6 5.0 COc1ccc(NS(=O)(=O)c2ccc(-c3c(C)cccc3C)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69197133 95734 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)s1 10.6019/CHEMBL2364335
CHEMBL2364421 95734 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)s1 10.6019/CHEMBL2364335
69197849 95759 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 429 5 2 5 4.1 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364445 95759 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 429 5 2 5 4.1 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69198350 95766 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 6 2 9 3.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csnn2)s1 10.6019/CHEMBL2364335
CHEMBL2364452 95766 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 6 2 9 3.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csnn2)s1 10.6019/CHEMBL2364335
156020452 184813 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 4 5 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@]3(C)C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4646979 184813 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 4 5 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@]3(C)C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
44579860 195680 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(C[C@H]1CCCN1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL507551 195680 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(C[C@H]1CCCN1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
145956415 168842 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160541 168842 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145956415 168842 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160541 168842 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145956753 168936 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4162000 168936 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145958774 169045 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163811 169045 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145955718 169314 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4167965 169314 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145952404 169515 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4171300 169515 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL3578014 218544 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
44436816 98580 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 524 12 4 6 3.9 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CCN)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL241242 98580 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 524 12 4 6 3.9 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CCN)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44391028 71072 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 451 9 1 4 3.9 CC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181051 71072 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 451 9 1 4 3.9 CC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44390906 138881 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 467 7 2 5 4.2 CC(C)(CN)CNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL369571 138881 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 467 7 2 5 4.2 CC(C)(CN)CNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
44434052 96191 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccc(NS(C)(=O)=O)cc1 10.1016/j.bmcl.2007.07.099
CHEMBL237059 96191 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccc(NS(C)(=O)=O)cc1 10.1016/j.bmcl.2007.07.099
44450169 166529 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 471 12 3 8 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCC(F)(F)F 10.1016/j.bmcl.2008.03.059
CHEMBL410499 166529 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 471 12 3 8 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCC(F)(F)F 10.1016/j.bmcl.2008.03.059
56926894 75839 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923638 75839 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
44391027 135581 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 541 12 1 4 5.6 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CCc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL366916 135581 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 541 12 1 4 5.6 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CCc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
44579803 193548 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(Cc1ccccc1Cl)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL488966 193548 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(Cc1ccccc1Cl)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
145952404 169515 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4171300 169515 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL3578014 218544 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
11526696 78377 17 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm1012374
CHEMBL1923502 78377 17 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm1012374
CHEMBL1963249 78377 17 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm1012374
44450045 166016 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 447 14 4 9 0.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL409894 166016 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 447 14 4 9 0.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCO 10.1016/j.bmcl.2008.03.059
44434012 95849 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 479 13 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL236513 95849 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 479 13 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCc1ccccc1 10.1016/j.bmcl.2007.07.099
44454398 104374 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(C#N)c1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL270851 104374 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(C#N)c1ccccc1 10.1016/j.bmcl.2008.01.100
11526745 75843 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923642 75843 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
44391020 70638 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 543 11 1 5 5.7 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OCc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180337 70638 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 543 11 1 5 5.7 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OCc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
162643920 188559 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 679 14 4 8 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4777792 188559 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 679 14 4 8 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
155540883 179736 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.41 +/- 0.13 nM)Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.41 +/- 0.13 nM)
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4517399 179736 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.41 +/- 0.13 nM)Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.41 +/- 0.13 nM)
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
145955718 169314 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4167965 169314 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
23648236 85927 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 524 13 3 7 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NCCN)c(OC)c1 10.1021/jm0704550
CHEMBL2113317 85927 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 524 13 3 7 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NCCN)c(OC)c1 10.1021/jm0704550
145958317 169092 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164531 169092 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
162649014 186720 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 702 14 4 7 6.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2c[nH]c3ccccc23)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4746362 186720 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 702 14 4 7 6.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2c[nH]c3ccccc23)cc1 10.1021/acs.jmedchem.9b02122
44434123 152328 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 343 8 2 8 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC#N 10.1016/j.bmcl.2007.07.099
CHEMBL391510 152328 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 343 8 2 8 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC#N 10.1016/j.bmcl.2007.07.099
11526696 78377 17 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923502 78377 17 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1963249 78377 17 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
122178179 128041 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1002 29 10 9 3.8 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
CHEMBL3578008 128041 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1002 29 10 9 3.8 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
145980382 173422 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4281310 173422 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
71453489 216147 15 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 216147 15 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
134149793 155384 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 5 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(CC)C1=O nan
CHEMBL3939196 155384 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 5 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(CC)C1=O nan
145980333 173360 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 577 6 1 4 7.5 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4280040 173360 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 577 6 1 4 7.5 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
44579823 190860 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL482420 190860 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
145957075 169058 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164040 169058 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
145951150 169555 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4171914 169555 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
44449864 165609 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 539 16 4 10 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1cccc(C(=O)NCCCCO)c1 10.1016/j.bmcl.2008.03.059
CHEMBL409462 165609 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 539 16 4 10 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1cccc(C(=O)NCCCCO)c1 10.1016/j.bmcl.2008.03.059
10005618 17095 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 11 1 3 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1 10.1016/j.bmc.2007.01.057
CHEMBL1162058 17095 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 11 1 3 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1 10.1016/j.bmc.2007.01.057
15481181 84519 2 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
CHEMBL209020 84519 2 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
9810101 106025 17 None 5 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL281764 106025 17 None 5 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
15481188 147988 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1016/j.bmc.2007.01.057
CHEMBL382844 147988 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1016/j.bmc.2007.01.057
CHEMBL130229 215466 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL None None None CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1016/j.bmc.2007.01.057
16114292 103709 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
CHEMBL266063 103709 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
16114292 103709 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL266063 103709 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
23730225 160955 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 435 12 4 10 -0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCO 10.1021/jm7010595
CHEMBL398570 160955 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 435 12 4 10 -0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCO 10.1021/jm7010595
10530781 22350 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 554 12 2 4 4.2 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL122108 22350 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 554 12 2 4 4.2 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
10005618 17095 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 11 1 3 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1 10.1016/j.bmc.2007.01.057
CHEMBL1162058 17095 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 11 1 3 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1 10.1016/j.bmc.2007.01.057
15481181 84519 2 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
CHEMBL209020 84519 2 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
9810101 106025 17 None 5 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL281764 106025 17 None 5 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
15481188 147988 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1016/j.bmc.2007.01.057
CHEMBL382844 147988 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1016/j.bmc.2007.01.057
CHEMBL130229 215466 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL None None None CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1016/j.bmc.2007.01.057
156011385 184157 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 518 8 3 5 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCCCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637916 184157 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 518 8 3 5 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCCCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44449956 103390 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 523 14 3 9 2.0 CN(CCc1cccc(O)c1)C(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
CHEMBL263389 103390 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 523 14 3 9 2.0 CN(CCc1cccc(O)c1)C(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
44447846 101674 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 547 15 4 11 1.2 CC(C)(N)C(=O)N[C@H](COCc1cccc(OC(F)(F)F)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254166 101674 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 547 15 4 11 1.2 CC(C)(N)C(=O)N[C@H](COCc1cccc(OC(F)(F)F)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44444566 161546 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 470 5 1 7 3.4 COc1cc2c(cc1N1CCN[C@@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL400124 161546 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 470 5 1 7 3.4 COc1cc2c(cc1N1CCN[C@@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
156011385 184157 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 518 8 3 5 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCCCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637916 184157 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 518 8 3 5 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCCCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156019457 184721 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645625 184721 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44570961 199340 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 421 4 1 5 2.2 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccco3)c(F)c2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL521246 199340 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 421 4 1 5 2.2 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccco3)c(F)c2)C1 10.1016/j.bmcl.2008.12.042
69195095 95738 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)c(F)c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364425 95738 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)c(F)c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69194503 95774 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)cc1Cl 10.6019/CHEMBL2364335
CHEMBL2364460 95774 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)cc1Cl 10.6019/CHEMBL2364335
59007103 95800 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 456 6 2 7 3.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cn1 10.6019/CHEMBL2364335
CHEMBL2364485 95800 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 456 6 2 7 3.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cn1 10.6019/CHEMBL2364335
69197358 95806 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 3 6 4.1 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3O)cc2F)o1 10.6019/CHEMBL2364335
CHEMBL2364491 95806 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 3 6 4.1 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3O)cc2F)o1 10.6019/CHEMBL2364335
44450046 102631 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 501 14 4 9 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCN1CCNC1=O 10.1016/j.bmcl.2008.03.059
CHEMBL259016 102631 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 501 14 4 9 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCN1CCNC1=O 10.1016/j.bmcl.2008.03.059
23730341 96517 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 502 11 3 10 0.1 CC(=O)N[C@@H]1CCN(C(=O)OCCn2nnnc2[C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)C1 10.1021/jm7010595
CHEMBL237701 96517 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 502 11 3 10 0.1 CC(=O)N[C@@H]1CCN(C(=O)OCCn2nnnc2[C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)C1 10.1021/jm7010595
71453489 216147 15 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Asp mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Asp mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 216147 15 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Asp mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Asp mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44390914 70412 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 11 1 5 4.9 CCCOC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180093 70412 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 11 1 5 4.9 CCCOC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
22888424 129776 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 541 11 1 4 5.7 CC(C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C)c1ccccc1 10.1016/j.bmcl.2005.02.040
CHEMBL360877 129776 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 541 11 1 4 5.7 CC(C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C)c1ccccc1 10.1016/j.bmcl.2005.02.040
71453489 216147 15 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 216147 15 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
162671996 189610 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 707 16 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)NCCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4791255 189610 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 707 16 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)NCCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
23730228 96367 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 477 14 3 10 0.6 CN(CCCCO)C(=O)OCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1021/jm7010595
CHEMBL237492 96367 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 477 14 3 10 0.6 CN(CCCCO)C(=O)OCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1021/jm7010595
71453489 216147 15 None - 1 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 216147 15 None - 1 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44444568 100753 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 470 5 1 7 3.4 COc1cc2c(cc1N1CCN[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL248542 100753 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 470 5 1 7 3.4 COc1cc2c(cc1N1CCN[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
15481185 84036 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
CHEMBL207970 84036 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
156011736 184202 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 605 7 3 7 3.0 Cc1oc(-c2ccc(C(F)(F)F)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4638566 184202 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 605 7 3 7 3.0 Cc1oc(-c2ccc(C(F)(F)F)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
25022506 102042 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 457 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL256263 102042 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 457 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2007.12.021
24803347 161807 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL401548 161807 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1 10.1016/j.bmcl.2007.12.021
46882394 12614 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 438 8 2 4 4.2 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cnc[nH]2)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1079185 12614 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 438 8 2 4 4.2 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cnc[nH]2)CC3)cc1 10.1016/j.bmcl.2009.09.027
46882395 12615 0 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 452 8 2 4 4.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2[nH]cnc2C)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1079186 12615 0 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 452 8 2 4 4.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2[nH]cnc2C)CC3)cc1 10.1016/j.bmcl.2009.09.027
44570699 198084 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 474 5 2 5 2.2 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(NC(=O)c3ccccc3F)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL519121 198084 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 474 5 2 5 2.2 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(NC(=O)c3ccccc3F)cc2)C1 10.1016/j.bmcl.2008.12.042
69196498 95686 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)s1 10.6019/CHEMBL2364335
CHEMBL2364374 95686 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)s1 10.6019/CHEMBL2364335
69197028 95725 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)c3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364413 95725 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)c3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69198238 95736 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 5 2 5 4.7 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364423 95736 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 5 2 5 4.7 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
11712867 95773 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)cc1F 10.6019/CHEMBL2364335
CHEMBL2364459 95773 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)cc1F 10.6019/CHEMBL2364335
69194471 95788 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)c(F)c1 10.6019/CHEMBL2364335
CHEMBL2364473 95788 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)c(F)c1 10.6019/CHEMBL2364335
11698505 95797 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)c2)cc1 10.6019/CHEMBL2364335
CHEMBL2364482 95797 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)c2)cc1 10.6019/CHEMBL2364335
9950632 95481 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.05.100
CHEMBL236038 95481 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.05.100
44579880 193614 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL489401 193614 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
44579841 199333 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccc(Cl)cc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL521176 199333 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccc(Cl)cc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44434010 95548 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 445 14 3 8 1.5 CCCCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
CHEMBL236311 95548 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 445 14 3 8 1.5 CCCCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
9950632 95481 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2007.07.099
9950632 95481 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.01.100
CHEMBL236038 95481 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2007.07.099
CHEMBL236038 95481 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.01.100
44434010 95548 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 445 14 3 8 1.5 CCCCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL236311 95548 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 445 14 3 8 1.5 CCCCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
44437966 208872 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 607 8 1 5 4.8 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N1CCOCC1)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
CHEMBL608827 208872 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 607 8 1 5 4.8 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N1CCOCC1)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
44437969 209298 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 565 8 1 4 5.0 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N(C)C)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
CHEMBL611488 209298 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 565 8 1 4 5.0 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N(C)C)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
44437966 208872 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 607 8 1 5 4.8 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N1CCOCC1)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
CHEMBL608827 208872 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 607 8 1 5 4.8 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N1CCOCC1)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
44437969 209298 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 565 8 1 4 5.0 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N(C)C)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
CHEMBL611488 209298 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 565 8 1 4 5.0 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N(C)C)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
44454368 102037 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCC(C#N)c2ccccc2)n1 10.1016/j.bmcl.2008.01.100
CHEMBL256236 102037 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCC(C#N)c2ccccc2)n1 10.1016/j.bmcl.2008.01.100
145987684 174056 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 615 6 1 4 7.8 CC[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4293331 174056 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 615 6 1 4 7.8 CC[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
44444560 161733 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 541 5 1 5 3.4 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)Cc1cccc(I)c1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL401133 161733 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 541 5 1 5 3.4 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)Cc1cccc(I)c1)CC2 10.1016/j.bmcl.2007.09.067
145953855 169294 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4167669 169294 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
44570923 190735 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 403 4 1 5 2.0 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccco3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL481602 190735 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 403 4 1 5 2.0 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccco3)cc2)C1 10.1016/j.bmcl.2008.12.042
44570761 196751 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 413 4 1 4 2.5 NC1CCN(C(=O)C2CCCCN2S(=O)(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL517081 196751 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 413 4 1 4 2.5 NC1CCN(C(=O)C2CCCCN2S(=O)(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
122178179 128041 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1002 29 10 9 3.8 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
CHEMBL3578008 128041 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1002 29 10 9 3.8 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
24969112 95651 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 445 5 2 7 3.2 Cc1ccc(-c2ccc(S(=O)(=O)Nc3ccnc(N4C[C@H](C)N[C@H](C)C4)n3)cc2F)o1 10.6019/CHEMBL2364335
CHEMBL2364339 95651 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 445 5 2 7 3.2 Cc1ccc(-c2ccc(S(=O)(=O)Nc3ccnc(N4C[C@H](C)N[C@H](C)C4)n3)cc2F)o1 10.6019/CHEMBL2364335
11540248 95657 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 479 5 2 6 4.9 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364345 95657 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 479 5 2 6 4.9 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11647560 95659 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 425 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2cccc3ccccc23)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364347 95659 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 425 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2cccc3ccccc23)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69196005 95690 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1sc2ccc(F)cc2c1C 10.6019/CHEMBL2364335
CHEMBL2364378 95690 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1sc2ccc(F)cc2c1C 10.6019/CHEMBL2364335
69198434 95698 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 488 7 2 8 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnccc2OC)s1 10.6019/CHEMBL2364335
CHEMBL2364386 95698 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 488 7 2 8 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnccc2OC)s1 10.6019/CHEMBL2364335
69198286 95706 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 401 4 2 5 3.9 C[C@H]1CN(c2cccc(NS(=O)(=O)c3cc4ccccc4s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364394 95706 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 401 4 2 5 3.9 C[C@H]1CN(c2cccc(NS(=O)(=O)c3cc4ccccc4s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11562181 95717 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 487 6 2 5 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(F)c3F)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364405 95717 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 487 6 2 5 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(F)c3F)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69196132 95728 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(F)c2)s1 10.6019/CHEMBL2364335
CHEMBL2364416 95728 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(F)c2)s1 10.6019/CHEMBL2364335
69197703 95729 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)cc2)s1 10.6019/CHEMBL2364335
CHEMBL2364417 95729 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)cc2)s1 10.6019/CHEMBL2364335
69194443 95750 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 487 6 2 5 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(F)c2F)cc1 10.6019/CHEMBL2364335
CHEMBL2364436 95750 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 487 6 2 5 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(F)c2F)cc1 10.6019/CHEMBL2364335
11503069 95753 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 439 5 2 4 4.5 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccccc4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364439 95753 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 439 5 2 4 4.5 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccccc4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11647941 95760 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.4 Cc1cc(-c2ccoc2)ccc1S(=O)(=O)Nc1cc(N2C[C@H](C)N[C@H](C)C2)ccc1F 10.6019/CHEMBL2364335
CHEMBL2364446 95760 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.4 Cc1cc(-c2ccoc2)ccc1S(=O)(=O)Nc1cc(N2C[C@H](C)N[C@H](C)C2)ccc1F 10.6019/CHEMBL2364335
11576203 95767 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 6 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2c(c1)CCC(C)(C)O2 10.6019/CHEMBL2364335
CHEMBL2364453 95767 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 6 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2c(c1)CCC(C)(C)O2 10.6019/CHEMBL2364335
11683891 95781 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 453 6 2 7 3.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnccn2)cc1 10.6019/CHEMBL2364335
CHEMBL2364467 95781 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 453 6 2 7 3.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnccn2)cc1 10.6019/CHEMBL2364335
69194380 95805 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 6 2 6 4.0 COc1ccc(N2CCN[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364490 95805 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 6 2 6 4.0 COc1ccc(N2CCN[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
56926783 75833 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 470 4 3 4 2.8 CC[C@H](C)[C@@H]1NCCCC/C=C/CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923632 75833 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 470 4 3 4 2.8 CC[C@H](C)[C@@H]1NCCCC/C=C/CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
156021183 184903 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648308 184903 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156017268 184429 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641472 184429 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156021183 184903 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648308 184903 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44453070 101868 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 453 6 2 7 3.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cncnc2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL255401 101868 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 453 6 2 7 3.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cncnc2)cc1 10.1016/j.bmcl.2007.12.021
44453097 161872 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 452 6 2 6 3.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccncc2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL401891 161872 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 452 6 2 6 3.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccncc2)cc1 10.1016/j.bmcl.2007.12.021
44570762 190207 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 414 4 1 5 1.9 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3cccnc3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL479865 190207 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 414 4 1 5 1.9 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3cccnc3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL3578013 218543 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
156017268 184429 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641472 184429 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44434114 96193 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 452 10 2 9 1.5 COC(=O)C(c1ccccc1)n1nnc([C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)n1 10.1016/j.bmcl.2007.07.099
CHEMBL237060 96193 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 452 10 2 9 1.5 COC(=O)C(c1ccccc1)n1nnc([C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)n1 10.1016/j.bmcl.2007.07.099
44450134 168671 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 479 13 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCc1ccccc1 10.1016/j.bmcl.2008.03.059
CHEMBL415095 168671 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 479 13 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCc1ccccc1 10.1016/j.bmcl.2008.03.059
44446177 101422 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252448 101422 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL500468 220894 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/s0960-894x(01)00324-9
44450105 102577 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 507 15 3 8 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCc1ccccc1 10.1016/j.bmcl.2008.03.059
CHEMBL258762 102577 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 507 15 3 8 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCc1ccccc1 10.1016/j.bmcl.2008.03.059
44447848 101675 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 547 15 4 11 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccc(OC(F)(F)F)cc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254167 101675 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 547 15 4 11 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccc(OC(F)(F)F)cc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44580031 199849 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 381 7 2 4 3.2 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL522446 199849 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 381 7 2 4 3.2 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL3578013 218543 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
44447845 101653 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 599 14 4 10 2.3 CC(C)(N)C(=O)N[C@H](COCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL253966 101653 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 599 14 4 10 2.3 CC(C)(N)C(=O)N[C@H](COCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44434119 96681 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 400 10 3 10 -0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1nnn[nH]1 10.1016/j.bmcl.2007.07.099
CHEMBL237925 96681 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 400 10 3 10 -0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1nnn[nH]1 10.1016/j.bmcl.2007.07.099
145953855 169294 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4167669 169294 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
44434121 96683 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 385 11 2 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCC#N 10.1016/j.bmcl.2007.07.099
CHEMBL237927 96683 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 385 11 2 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCC#N 10.1016/j.bmcl.2007.07.099
162646324 186515 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 688 17 3 9 4.8 CCN(CC)CCc1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(OC)cc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4744139 186515 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 688 17 3 9 4.8 CCN(CC)CCc1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(OC)cc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
10721075 22325 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 534 11 2 5 3.8 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1csc2ccccc12)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL121960 22325 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 534 11 2 5 3.8 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1csc2ccccc12)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
145959787 169064 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 169064 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
16114289 105441 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCNC2)cc1 10.1021/jm0704550
CHEMBL277376 105441 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCNC2)cc1 10.1021/jm0704550
56926892 75837 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923636 75837 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
145984632 173170 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 629 5 1 4 8.0 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)C(C)(C)C2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4276775 173170 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 629 5 1 4 8.0 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)C(C)(C)C2)ncn1 10.1021/acs.jmedchem.8b00794
155551597 180728 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 974 27 13 11 -1.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4541252 180728 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 974 27 13 11 -1.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
22862448 103953 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CC(=O)c1ccccc1O2 10.1016/s0960-894x(97)10199-8
CHEMBL268231 103953 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CC(=O)c1ccccc1O2 10.1016/s0960-894x(97)10199-8
22867465 103994 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)Cc1ccccc1C2 10.1016/s0960-894x(97)10199-8
CHEMBL268518 103994 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)Cc1ccccc1C2 10.1016/s0960-894x(97)10199-8
44301387 18036 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1179088 18036 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL59572 18036 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
56926356 75794 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923512 75794 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
10143731 71102 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 543 11 2 5 4.7 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)C(O)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181156 71102 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 543 11 2 5 4.7 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)C(O)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
44444558 174556 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 465 4 0 5 4.1 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(S(=O)(=O)c1ccc3ccccc3c1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL430398 174556 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 465 4 0 5 4.1 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(S(=O)(=O)c1ccc3ccccc3c1)CC2 10.1016/j.bmcl.2007.09.067
145959007 169036 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163623 169036 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
145959787 169064 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 169064 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
156021766 184906 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648355 184906 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44452826 102157 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 428 5 2 6 3.8 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
CHEMBL256809 102157 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 428 5 2 6 3.8 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
44452777 102995 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 470 6 2 7 4.0 CC(=O)c1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
CHEMBL260831 102995 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 470 6 2 7 4.0 CC(=O)c1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
11554351 103314 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 458 6 2 6 2.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(N2CCCC2=O)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL262879 103314 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 458 6 2 6 2.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(N2CCCC2=O)cc1 10.1016/j.bmcl.2007.12.021
11605061 103489 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 462 5 2 6 4.5 C[C@H]1CN(c2ccc(Cl)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
CHEMBL264170 103489 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 462 5 2 6 4.5 C[C@H]1CN(c2ccc(Cl)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
44452825 162029 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 472 7 2 7 4.2 CCOc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
CHEMBL402772 162029 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 472 7 2 7 4.2 CCOc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
CHEMBL3578017 218547 0 None -3 2 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
69197033 95682 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 442 6 2 7 3.3 COc1ccc(NS(=O)(=O)c2ccc(-c3cnco3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364370 95682 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 442 6 2 7 3.3 COc1ccc(NS(=O)(=O)c2ccc(-c3cnco3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69197513 95697 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 448 6 2 8 3.4 COc1ccc(NS(=O)(=O)c2ccc(-c3cnco3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364385 95697 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 448 6 2 8 3.4 COc1ccc(NS(=O)(=O)c2ccc(-c3cnco3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69196509 95701 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 467 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2C)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364389 95701 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 467 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2C)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11669948 95713 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 467 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2ccc(Br)c(C)c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364401 95713 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 467 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2ccc(Br)c(C)c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69196071 95771 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 478 6 2 8 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)n2)s1 10.6019/CHEMBL2364335
CHEMBL2364457 95771 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 478 6 2 8 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)n2)s1 10.6019/CHEMBL2364335
69194899 95775 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2ccoc2)c1 10.6019/CHEMBL2364335
CHEMBL2364461 95775 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2ccoc2)c1 10.6019/CHEMBL2364335
44434055 96080 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL236858 96080 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
44436889 159836 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 563 11 3 5 6.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCCCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL397594 159836 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 563 11 3 5 6.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCCCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44570922 199342 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 415 3 1 4 1.6 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL521264 199342 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 415 3 1 4 1.6 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.12.042
69196838 95662 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 426 5 2 6 3.2 COc1ccc(NS(=O)(=O)c2cccc3cccnc23)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364350 95662 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 426 5 2 6 3.2 COc1ccc(NS(=O)(=O)c2cccc3cccnc23)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
25211977 193681 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 C[C@H](Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL489818 193681 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 C[C@H](Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
16113580 144657 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm701292s
CHEMBL376258 144657 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm701292s
44434111 153061 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1cc2ccccc2n1S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL392077 153061 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1cc2ccccc2n1S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
15481185 84036 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
CHEMBL207970 84036 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
127048059 146344 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 675 16 6 8 4.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797225 146344 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 675 16 6 8 4.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
16113580 144657 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL376258 144657 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
44450103 102547 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 495 14 3 10 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCS(C)(=O)=O 10.1016/j.bmcl.2008.03.059
CHEMBL258551 102547 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 495 14 3 10 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCS(C)(=O)=O 10.1016/j.bmcl.2008.03.059
44391032 71619 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 513 8 1 5 5.7 CC(C)N(CCNC(=O)C1c2ccc(Oc3cccc(F)c3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL182050 71619 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 513 8 1 5 5.7 CC(C)N(CCNC(=O)C1c2ccc(Oc3cccc(F)c3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
156011736 184202 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 605 7 3 7 3.0 Cc1oc(-c2ccc(C(F)(F)F)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4638566 184202 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 605 7 3 7 3.0 Cc1oc(-c2ccc(C(F)(F)F)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
44450132 102787 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 447 14 4 9 0.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCNC(=O)CCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL259712 102787 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 447 14 4 9 0.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCNC(=O)CCCCO 10.1016/j.bmcl.2008.03.059
145948725 174276 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 885 20 7 9 6.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL4299615 174276 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 885 20 7 9 6.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
44281450 106421 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 573 12 3 8 1.5 COC(=O)CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
CHEMBL284295 106421 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 573 12 3 8 1.5 COC(=O)CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
44281450 106421 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 573 12 3 8 1.5 COC(=O)CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
CHEMBL284295 106421 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 573 12 3 8 1.5 COC(=O)CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
44411584 17075 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161822 17075 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
156015766 184347 0 None 407 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 7 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4640438 184347 0 None 407 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 7 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2)on1 10.1021/acs.jmedchem.0c00828
44411584 17075 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161822 17075 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
22888433 71387 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 535 10 1 5 5.9 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC1CCCCC1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181735 71387 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 535 10 1 5 5.9 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC1CCCCC1)C(C)C 10.1016/j.bmcl.2005.02.040
44579775 193959 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 352 7 1 3 3.5 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1ccccc1 10.1016/j.bmcl.2008.07.120
CHEMBL492230 193959 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 352 7 1 3 3.5 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1ccccc1 10.1016/j.bmcl.2008.07.120
11258291 195883 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1Cl)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL510195 195883 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1Cl)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44579882 199845 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL522426 199845 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
44450044 167881 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 433 13 4 9 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCO 10.1016/j.bmcl.2008.03.059
CHEMBL411699 167881 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 433 13 4 9 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCO 10.1016/j.bmcl.2008.03.059
56926463 75813 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923611 75813 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
145981687 173356 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 509 5 1 3 6.5 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(Cl)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4279987 173356 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 509 5 1 3 6.5 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(Cl)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
44579640 193675 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 354 7 1 4 3.2 COc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
CHEMBL489793 193675 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 354 7 1 4 3.2 COc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
44579686 193770 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 395 8 2 4 3.6 CCC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(NC(C)=O)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL490614 193770 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 395 8 2 4 3.6 CCC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(NC(C)=O)cc1 10.1016/j.bmcl.2008.07.120
16203238 143887 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 531 9 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1 10.1021/jm070024h
CHEMBL374757 143887 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 531 9 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1 10.1021/jm070024h
44390997 129779 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 481 8 1 5 4.6 CC(C)N(C)CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL360891 129779 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 481 8 1 5 4.6 CC(C)N(C)CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL3578017 218547 0 None -3 2 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
23661656 175823 0 None -7 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 564 8 1 4 5.3 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
CHEMBL439560 175823 0 None -7 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 564 8 1 4 5.3 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
44434074 161452 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL399625 161452 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
44434009 174232 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 431 13 3 8 1.1 CCCCNC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL429799 174232 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 431 13 3 8 1.1 CCCCNC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
22867312 30642 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 472 5 3 4 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)Cc1ccccc1C2=O 10.1016/s0960-894x(97)10199-8
CHEMBL13366 30642 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 472 5 3 4 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)Cc1ccccc1C2=O 10.1016/s0960-894x(97)10199-8
162665952 189158 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 688 14 4 10 3.5 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4785149 189158 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 688 14 4 10 3.5 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
44434056 151773 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL391088 151773 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
44434007 95350 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 390 10 2 9 0.3 COC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL235446 95350 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 390 10 2 9 0.3 COC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
156021766 184906 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648355 184906 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44391035 129386 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 545 11 1 4 5.3 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)Cc1ccccc1F)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL360247 129386 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 545 11 1 4 5.3 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)Cc1ccccc1F)C(C)C 10.1016/j.bmcl.2005.02.040
44301512 18794 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 566 13 3 8 1.0 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@@H](N)CO)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1183340 18794 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 566 13 3 8 1.0 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@@H](N)CO)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL291333 18794 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 566 13 3 8 1.0 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@@H](N)CO)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
145979268 173443 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 607 8 1 5 7.4 COc1ccc([C@H](CC2CC2)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4281647 173443 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 607 8 1 5 7.4 COc1ccc([C@H](CC2CC2)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
145959007 169036 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163623 169036 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
44580030 193749 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 324 6 1 3 3.2 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccccc1 10.1016/j.bmcl.2008.07.120
CHEMBL490422 193749 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 324 6 1 3 3.2 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccccc1 10.1016/j.bmcl.2008.07.120
118718706 122157 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL3350011 122157 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
44301462 18034 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1179075 18034 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL58758 18034 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
16113800 144590 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 536 11 3 6 4.7 COc1cccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL375972 144590 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 536 11 3 6 4.7 COc1cccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
44391015 130333 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 1 5 5.2 COc1ccc(CC(=O)N2CCc3cc(OCc4ccccc4)ccc3C2C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
CHEMBL361802 130333 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 1 5 5.2 COc1ccc(CC(=O)N2CCc3cc(OCc4ccccc4)ccc3C2C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
162677268 190352 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 663 14 3 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4800459 190352 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 663 14 3 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
10507433 23239 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 578 13 3 6 3.5 C[C@H](O)CNC(=O)[C@@H](Cc1cccs1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL123430 23239 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 578 13 3 6 3.5 C[C@H](O)CNC(=O)[C@@H](Cc1cccs1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
23730458 153350 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 499 14 3 11 0.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCn1ccnc1 10.1021/jm7010595
CHEMBL392296 153350 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 499 14 3 11 0.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCn1ccnc1 10.1021/jm7010595
44576247 221001 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL506986 221001 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
168285897 198436 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 273 7 1 2 4.1 CCCCCCCc1cc(=O)c2cc(OC)ccc2[nH]1 10.1021/acs.jmedchem.1c02191
CHEMBL5196194 198436 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 273 7 1 2 4.1 CCCCCCCc1cc(=O)c2cc(OC)ccc2[nH]1 10.1021/acs.jmedchem.1c02191
155529391 178219 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1427 41 20 17 -3.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4463042 178219 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1427 41 20 17 -3.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
145956659 168834 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4160434 168834 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
155537651 179095 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1597 47 22 19 -3.8 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(N)=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4475293 179095 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1597 47 22 19 -3.8 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(N)=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
145981196 173315 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 627 5 1 6 7.1 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)N[C@@H](C)c4ccc(-c5cnccn5)c(Cl)c4Cl)CC3)C2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4279344 173315 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 627 5 1 6 7.1 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)N[C@@H](C)c4ccc(-c5cnccn5)c(Cl)c4Cl)CC3)C2)ncn1 10.1021/acs.jmedchem.8b00794
145979819 173252 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 655 8 1 6 7.9 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4278185 173252 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 655 8 1 6 7.9 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
44434016 96968 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 415 12 3 7 1.5 CCCCNC(=O)CCn1nnnc1[C@@H](CCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL238228 96968 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 415 12 3 7 1.5 CCCCNC(=O)CCn1nnnc1[C@@H](CCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
16113692 144014 1 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 559 11 4 5 5.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
CHEMBL375162 144014 1 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 559 11 4 5 5.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
24970113 75831 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 580 3 3 5 3.8 C[C@@H]1CN[C@@H](C2CCCCC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923629 75831 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 580 3 3 5 3.8 C[C@@H]1CN[C@@H](C2CCCCC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL2170777 216144 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CCC[C@H](NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm300414b
145956026 169441 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4169979 169441 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
22862436 17086 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161834 17086 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
10602640 144967 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1016/j.bmc.2007.01.057
CHEMBL376970 144967 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1016/j.bmc.2007.01.057
10791616 146314 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL379564 146314 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
10029990 176063 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL441360 176063 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
11526696 78377 17 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release incubated for 3 mins by FLIPR assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release incubated for 3 mins by FLIPR assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
CHEMBL1923502 78377 17 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release incubated for 3 mins by FLIPR assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release incubated for 3 mins by FLIPR assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
CHEMBL1963249 78377 17 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release incubated for 3 mins by FLIPR assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release incubated for 3 mins by FLIPR assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
10649323 22302 0 None - 1 Rat 8.3 pEC50 = 8.3 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 508 13 2 5 2.5 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](COCc1ccccc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL121803 22302 0 None - 1 Rat 8.3 pEC50 = 8.3 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 508 13 2 5 2.5 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](COCc1ccccc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
10841400 23623 0 None - 1 Rat 8.3 pEC50 = 8.3 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 608 13 3 5 3.7 C[C@H](O)CNC(=O)[C@@H](Cc1ccc(F)c(F)c1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL124831 23623 0 None - 1 Rat 8.3 pEC50 = 8.3 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 608 13 3 5 3.7 C[C@H](O)CNC(=O)[C@@H](Cc1ccc(F)c(F)c1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
156009875 183902 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633695 183902 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44444562 101246 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 463 6 1 5 3.5 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)CCc1ccccc1Cl)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL251365 101246 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 463 6 1 5 3.5 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)CCc1ccccc1Cl)CC2 10.1016/j.bmcl.2007.09.067
145956026 169441 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4169979 169441 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
22862436 17086 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161834 17086 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
10602640 144967 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1016/j.bmc.2007.01.057
CHEMBL376970 144967 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1016/j.bmc.2007.01.057
10791616 146314 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL379564 146314 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
10029990 176063 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL441360 176063 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
156009875 183902 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633695 183902 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156015766 184347 0 None 407 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 7 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4640438 184347 0 None 407 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 7 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2)on1 10.1021/acs.jmedchem.0c00828
44570967 196948 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 437 4 2 6 1.1 Cc1ccc(-c2ccc(S(=O)(=O)N3C[C@@H](O)C[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL517391 196948 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 437 4 2 6 1.1 Cc1ccc(-c2ccc(S(=O)(=O)N3C[C@@H](O)C[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
24969114 95654 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 506 6 2 7 4.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)nc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)cc1Cl 10.6019/CHEMBL2364335
CHEMBL2364342 95654 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 506 6 2 7 4.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)nc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)cc1Cl 10.6019/CHEMBL2364335
59007076 95677 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)cc1 10.6019/CHEMBL2364335
CHEMBL2364365 95677 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)cc1 10.6019/CHEMBL2364335
69197196 95679 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)s1 10.6019/CHEMBL2364335
CHEMBL2364367 95679 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)s1 10.6019/CHEMBL2364335
69197071 95718 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 445 5 2 5 4.5 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364406 95718 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 445 5 2 5 4.5 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69194482 95733 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 409 4 2 4 4.1 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2ccccc2c1 10.6019/CHEMBL2364335
CHEMBL2364420 95733 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 409 4 2 4 4.1 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2ccccc2c1 10.6019/CHEMBL2364335
11719784 95770 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)cc1C 10.6019/CHEMBL2364335
CHEMBL2364456 95770 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)cc1C 10.6019/CHEMBL2364335
59007054 95802 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 5 3 6 3.9 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3O)cc2)o1 10.6019/CHEMBL2364335
CHEMBL2364487 95802 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 5 3 6 3.9 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3O)cc2)o1 10.6019/CHEMBL2364335
16114097 85932 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCCNC2)c(OC)c1 10.1021/jm0704550
CHEMBL2113321 85932 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCCNC2)c(OC)c1 10.1021/jm0704550
16113710 85936 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCNCC1 10.1021/jm0704550
CHEMBL2113325 85936 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCNCC1 10.1021/jm0704550
23730226 154650 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 449 13 4 10 -0.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCO 10.1021/jm7010595
CHEMBL393329 154650 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 449 13 4 10 -0.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCO 10.1021/jm7010595
71453489 216147 15 None - 1 Human 8.3 pEC50 = 8.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.8b01644
CHEMBL2170781 216147 15 None - 1 Human 8.3 pEC50 = 8.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.8b01644
44411632 17076 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161823 17076 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
22888425 69298 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 2 5 4.7 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)C(CO)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL178216 69298 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 2 5 4.7 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)C(CO)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
44411632 17076 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161823 17076 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL2170782 216148 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1csc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44579858 193704 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2Cl)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL490010 193704 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2Cl)cc1 10.1016/j.bmcl.2008.07.120
44579778 193798 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1)C(=O)N(Cc1cccc(Cl)c1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL490801 193798 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1)C(=O)N(Cc1cccc(Cl)c1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
162657606 187896 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 693 15 3 8 5.7 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4760409 187896 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 693 15 3 8 5.7 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
145956659 168834 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4160434 168834 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
145950987 169619 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 4 3 5 1.7 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCO3)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4172848 169619 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 4 3 5 1.7 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCO3)ccc21 10.1021/acs.jmedchem.8b00322
69198313 95673 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 426 5 2 6 3.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc2cccnc12 10.6019/CHEMBL2364335
CHEMBL2364361 95673 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 426 5 2 6 3.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc2cccnc12 10.6019/CHEMBL2364335
69195692 95674 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.6019/CHEMBL2364335
CHEMBL2364362 95674 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.6019/CHEMBL2364335
69196612 95675 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 442 6 2 7 3.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnco2)cc1 10.6019/CHEMBL2364335
CHEMBL2364363 95675 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 442 6 2 7 3.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnco2)cc1 10.6019/CHEMBL2364335
11511158 95723 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccc3C)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364411 95723 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccc3C)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69198054 95776 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2cc(C)cs2)c1 10.6019/CHEMBL2364335
CHEMBL2364462 95776 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2cc(C)cs2)c1 10.6019/CHEMBL2364335
69195074 95789 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)nc1 10.6019/CHEMBL2364335
CHEMBL2364474 95789 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)nc1 10.6019/CHEMBL2364335
69195546 95799 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Cl)c2ccccc12 10.6019/CHEMBL2364335
CHEMBL2364484 95799 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Cl)c2ccccc12 10.6019/CHEMBL2364335
44580028 200029 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 416 8 1 4 4.5 COc1c(-c2ccccc2)cccc1N(C[C@H]1CCCN1)C(=O)COc1ccccc1 10.1016/j.bmcl.2008.07.120
CHEMBL523786 200029 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 416 8 1 4 4.5 COc1c(-c2ccccc2)cccc1N(C[C@H]1CCCN1)C(=O)COc1ccccc1 10.1016/j.bmcl.2008.07.120
44434011 154642 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 465 12 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL393321 154642 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 465 12 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCc1ccccc1 10.1016/j.bmcl.2007.07.099
57390496 75830 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
CHEMBL1923628 75830 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
145988894 173923 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4290680 173923 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
44434086 155634 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 420 10 2 7 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C/C=C/c2ccccc2)n1 10.1016/j.bmcl.2007.07.099
CHEMBL394130 155634 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 420 10 2 7 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C/C=C/c2ccccc2)n1 10.1016/j.bmcl.2007.07.099
145950987 169619 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 4 3 5 1.7 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCO3)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4172848 169619 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 4 3 5 1.7 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCO3)ccc21 10.1021/acs.jmedchem.8b00322
44449924 166724 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 487 12 4 9 1.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)N[C@H]1CC[C@H](O)CC1 10.1016/j.bmcl.2008.03.059
CHEMBL410730 166724 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 487 12 4 9 1.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)N[C@H]1CC[C@H](O)CC1 10.1016/j.bmcl.2008.03.059
56926785 75835 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923634 75835 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
44434078 96685 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 513 10 2 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CC2Cc3ccccc3N2S(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL237932 96685 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 513 10 2 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CC2Cc3ccccc3N2S(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
44434008 153312 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 404 11 2 9 0.7 COC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL392268 153312 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 404 11 2 9 0.7 COC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
44411913 17085 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161833 17085 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
44268939 37220 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@]2(CC(=O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
CHEMBL13926 37220 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@]2(CC(=O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
44411913 17085 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161833 17085 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
44434015 95266 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 493 14 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL235011 95266 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 493 14 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCCc1ccccc1 10.1016/j.bmcl.2007.07.099
44411905 17084 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161832 17084 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
10506325 108018 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1016/j.bmc.2007.01.057
CHEMBL296104 108018 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1016/j.bmc.2007.01.057
16113371 85928 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL2113318 85928 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
162676229 190083 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 715 15 3 10 3.9 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4797064 190083 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 715 15 3 10 3.9 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL3578005 218538 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1021/jm501702q
44348031 119866 0 None - 1 Rat 8.2 pEC50 = 8.2 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 618 14 3 5 4.3 C[C@@H](O)CNC(=O)[C@@H](Cc1ccc(F)cc1)N(C)C(=O)[C@@H](CC1=CCC(c2ccccc2)C=C1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL331303 119866 0 None - 1 Rat 8.2 pEC50 = 8.2 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 618 14 3 5 4.3 C[C@@H](O)CNC(=O)[C@@H](Cc1ccc(F)cc1)N(C)C(=O)[C@@H](CC1=CCC(c2ccccc2)C=C1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
44411905 17084 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161832 17084 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
44437953 17096 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 522 9 3 6 1.5 NCCNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCN1C(=O)CCS(=O)(=O)c2ccccc21 10.1016/j.bmc.2007.01.057
CHEMBL1162062 17096 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 522 9 3 6 1.5 NCCNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCN1C(=O)CCS(=O)(=O)c2ccccc21 10.1016/j.bmc.2007.01.057
10506325 108018 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1016/j.bmc.2007.01.057
CHEMBL296104 108018 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1016/j.bmc.2007.01.057
44436857 152434 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 594 12 4 7 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL391588 152434 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 594 12 4 7 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
156021787 184922 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648799 184922 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
10006735 123791 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 515 10 3 6 2.0 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(C)(=O)=O)CC1 10.1016/j.bmc.2007.01.057
CHEMBL33892 123791 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 515 10 3 6 2.0 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(C)(=O)=O)CC1 10.1016/j.bmc.2007.01.057
10006735 123791 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 515 10 3 6 2.0 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(C)(=O)=O)CC1 10.1016/j.bmc.2007.01.057
CHEMBL33892 123791 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 515 10 3 6 2.0 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(C)(=O)=O)CC1 10.1016/j.bmc.2007.01.057
156021787 184922 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648799 184922 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
11712108 168087 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 451 6 2 5 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL412303 168087 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 451 6 2 5 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2007.12.021
44571003 199367 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 445 4 1 5 3.0 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3C[C@H](C)N[C@H](C)C3)cc2)o1 10.1016/j.bmcl.2008.12.042
CHEMBL521439 199367 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 445 4 1 5 3.0 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3C[C@H](C)N[C@H](C)C3)cc2)o1 10.1016/j.bmcl.2008.12.042
CHEMBL3578005 218538 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1021/jm501702q
69196876 95664 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 7 2.9 COc1ccc(NS(=O)(=O)c2ccc(-n3cccn3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364352 95664 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 7 2.9 COc1ccc(NS(=O)(=O)c2ccc(-n3cccn3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11562329 95703 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 495 8 2 6 4.5 COCc1cccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)cc2)c1 10.6019/CHEMBL2364335
CHEMBL2364391 95703 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 495 8 2 6 4.5 COCc1cccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)cc2)c1 10.6019/CHEMBL2364335
69196868 95707 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 427 5 2 5 4.4 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-c4cccs4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364395 95707 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 427 5 2 5 4.4 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-c4cccs4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69196990 95763 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 480 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)cc1C 10.6019/CHEMBL2364335
CHEMBL2364449 95763 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 480 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)cc1C 10.6019/CHEMBL2364335
69195880 95780 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 6 5.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)c(C)c1 10.6019/CHEMBL2364335
CHEMBL2364466 95780 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 6 5.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)c(C)c1 10.6019/CHEMBL2364335
11518463 95783 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1cc(-c2cc(C)cs2)ccc1S(=O)(=O)Nc1cccc(N2C[C@H](C)N[C@H](C)C2)c1 10.6019/CHEMBL2364335
CHEMBL2364469 95783 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1cc(-c2cc(C)cs2)ccc1S(=O)(=O)Nc1cccc(N2C[C@H](C)N[C@H](C)C2)c1 10.6019/CHEMBL2364335
69195024 95807 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 461 5 3 6 4.2 C[C@H]1CN(c2ccc(O)c(NS(=O)(=O)c3ccc(-c4ccccc4F)s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364492 95807 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 461 5 3 6 4.2 C[C@H]1CN(c2ccc(O)c(NS(=O)(=O)c3ccc(-c4ccccc4F)s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
44390922 128924 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 1 5 5.2 COc1cccc(CC(=O)N2CCc3cc(OCc4ccccc4)ccc3C2C(=O)NCCN(C(C)C)C(C)C)c1 10.1016/j.bmcl.2005.02.040
CHEMBL359686 128924 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 1 5 5.2 COc1cccc(CC(=O)N2CCc3cc(OCc4ccccc4)ccc3C2C(=O)NCCN(C(C)C)C(C)C)c1 10.1016/j.bmcl.2005.02.040
23631026 174235 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant GHSR1a expressed in HEK293F cells assessed as stimulation of [35S]GTP-gamma-S binding relative to ghrelinAgonist activity at human recombinant GHSR1a expressed in HEK293F cells assessed as stimulation of [35S]GTP-gamma-S binding relative to ghrelin
ChEMBL 443 5 1 5 5.3 Cc1ccccc1-c1nc2ccc(Oc3ccc(F)cc3)cc2c(=O)n1CC1CCCNC1 10.1021/jm070071+
CHEMBL429817 174235 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant GHSR1a expressed in HEK293F cells assessed as stimulation of [35S]GTP-gamma-S binding relative to ghrelinAgonist activity at human recombinant GHSR1a expressed in HEK293F cells assessed as stimulation of [35S]GTP-gamma-S binding relative to ghrelin
ChEMBL 443 5 1 5 5.3 Cc1ccccc1-c1nc2ccc(Oc3ccc(F)cc3)cc2c(=O)n1CC1CCCNC1 10.1021/jm070071+
CHEMBL2170779 216145 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FLAG-tagged human ghrelin receptor Ser123:Ala mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at FLAG-tagged human ghrelin receptor Ser123:Ala mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44447842 101794 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.6 CC(C)(N)C(=O)N[C@H](COCc1cc(Cl)cc(Cl)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254972 101794 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.6 CC(C)(N)C(=O)N[C@H](COCc1cc(Cl)cc(Cl)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44579804 193844 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(Cc1ccc(Cl)cc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL491220 193844 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(Cc1ccc(Cl)cc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
145948708 174275 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 886 20 7 10 5.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CNCCO3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL4299606 174275 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 886 20 7 10 5.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CNCCO3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
121879 9015 24 None 1 5 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1016/s0960-894x(97)10199-8
5868 9015 24 None 1 5 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1016/s0960-894x(97)10199-8
CHEMBL308716 9015 24 None 1 5 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1016/s0960-894x(97)10199-8
44268996 173242 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(Cc3ccccc3C2)C1 10.1016/s0960-894x(97)10199-8
CHEMBL427806 173242 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(Cc3ccccc3C2)C1 10.1016/s0960-894x(97)10199-8
122178180 128042 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1130 35 12 11 3.4 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
CHEMBL3578009 128042 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1130 35 12 11 3.4 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
44579959 191051 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL483865 191051 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.120
44454117 162335 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
CHEMBL404336 162335 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
162677361 190288 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 685 16 4 8 4.7 COc1ccc(C[C@@H](N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4799766 190288 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 685 16 4 8 4.7 COc1ccc(C[C@@H](N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL2170700 216139 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc(C(C)(C)C)cc1)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44444570 161547 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 456 5 1 7 3.0 COc1cc2c(cc1N1CCNCC1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL400125 161547 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 456 5 1 7 3.0 COc1cc2c(cc1N1CCNCC1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
156017532 184687 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645072 184687 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
11662746 104589 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 467 7 2 6 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL271947 104589 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 467 7 2 6 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.12.021
122178180 128042 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1130 35 12 11 3.4 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
CHEMBL3578009 128042 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1130 35 12 11 3.4 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
CHEMBL3578007 218540 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm501702q
16750162 95653 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 474 6 2 7 3.8 COc1ncc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)c(F)c1 10.6019/CHEMBL2364335
CHEMBL2364341 95653 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 474 6 2 7 3.8 COc1ncc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)c(F)c1 10.6019/CHEMBL2364335
11568467 95663 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.0 COc1ccc(NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364351 95663 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.0 COc1ccc(NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69197136 95764 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc(C)c(-c2ccccc2F)s1 10.6019/CHEMBL2364335
CHEMBL2364450 95764 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc(C)c(-c2ccccc2F)s1 10.6019/CHEMBL2364335
69195304 95778 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 455 4 2 4 3.9 Cc1cc(S(=O)(=O)Nc2cc(N3C[C@H](C)N[C@H](C)C3)ccc2F)ccc1Br 10.6019/CHEMBL2364335
CHEMBL2364464 95778 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 455 4 2 4 3.9 Cc1cc(S(=O)(=O)Nc2cc(N3C[C@H](C)N[C@H](C)C3)ccc2F)ccc1Br 10.6019/CHEMBL2364335
145949880 169570 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4172217 169570 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
16114099 144002 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 559 10 4 5 5.5 Cc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL375103 144002 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 559 10 4 5 5.5 Cc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
44269018 104123 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CCc3ccccc32)C1 10.1016/s0960-894x(97)10199-8
CHEMBL269447 104123 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CCc3ccccc32)C1 10.1016/s0960-894x(97)10199-8
145949880 169570 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4172217 169570 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
156015598 184356 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 486 7 4 6 0.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(C2CC2)n[nH]1 10.1021/acs.jmedchem.0c00828
CHEMBL4640573 184356 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 486 7 4 6 0.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(C2CC2)n[nH]1 10.1021/acs.jmedchem.0c00828
44452827 102201 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 453 5 2 7 3.7 C[C@H]1CN(c2cc(NS(=O)(=O)c3ccc(-c4ccccn4)s3)ccc2C#N)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
CHEMBL257019 102201 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 453 5 2 7 3.7 C[C@H]1CN(c2cc(NS(=O)(=O)c3ccc(-c4ccccn4)s3)ccc2C#N)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
46882582 12527 0 None -125 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 466 5 2 5 3.9 CC1(C)CCc2cc(S(=O)(=O)Nc3ccc4c(c3)CCN(Cc3cc[nH]n3)CC4)ccc2O1 10.1016/j.bmcl.2009.09.027
CHEMBL1078490 12527 0 None -125 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 466 5 2 5 3.9 CC1(C)CCc2cc(S(=O)(=O)Nc3ccc4c(c3)CCN(Cc3cc[nH]n3)CC4)ccc2O1 10.1016/j.bmcl.2009.09.027
145988647 173851 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4ncccn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4289530 173851 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4ncccn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
44454367 102036 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
CHEMBL256235 102036 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
16113691 143497 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm0704550
CHEMBL374073 143497 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm0704550
16113691 143497 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
CHEMBL374073 143497 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
22867380 36193 1 None - 1 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 472 5 3 3 3.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCCc3ccccc32)CC1 10.1016/s0960-894x(97)10199-8
CHEMBL13841 36193 1 None - 1 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 472 5 3 3 3.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCCc3ccccc32)CC1 10.1016/s0960-894x(97)10199-8
2098 10466 36 None -128 11 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02122
36511 10466 36 None -128 11 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02122
3805 10466 36 None -128 11 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02122
3835 10466 36 None -128 11 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02122
CHEMBL235363 10466 36 None -128 11 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02122
155561671 182443 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 817 22 11 9 -0.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4581511 182443 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 817 22 11 9 -0.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
44434073 96375 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL237507 96375 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
145981794 173475 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 567 6 1 5 6.6 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4282394 173475 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 567 6 1 5 6.6 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
56926173 75787 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm1012374
CHEMBL1923501 75787 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm1012374
44301389 18047 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1179118 18047 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL61292 18047 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
156015598 184356 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 486 7 4 6 0.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(C2CC2)n[nH]1 10.1021/acs.jmedchem.0c00828
CHEMBL4640573 184356 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 486 7 4 6 0.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(C2CC2)n[nH]1 10.1021/acs.jmedchem.0c00828
156017532 184687 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645072 184687 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
10100708 18806 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 530 9 3 7 0.3 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@@H](N)CO)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL1183387 18806 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 530 9 3 7 0.3 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@@H](N)CO)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL294408 18806 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 530 9 3 7 0.3 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@@H](N)CO)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
44579756 193602 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL489370 193602 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
145958487 168963 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc(F)c21 10.1021/acs.jmedchem.8b00322
CHEMBL4162545 168963 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc(F)c21 10.1021/acs.jmedchem.8b00322
156016840 184410 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 621 7 3 7 3.4 Cc1nc(-c2cccc(C(F)(F)F)c2)sc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4641215 184410 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 621 7 3 7 3.4 Cc1nc(-c2cccc(C(F)(F)F)c2)sc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL2170779 216145 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at FLAG-tagged human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at FLAG-tagged human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
71453489 216147 15 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Thr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Thr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 216147 15 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Thr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Thr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
10209618 70273 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 555 11 1 5 5.4 CC(=O)c1ccccc1C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL179978 70273 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 555 11 1 5 5.4 CC(=O)c1ccccc1C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44391041 71095 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 591 11 1 6 5.1 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)S(=O)(=O)Cc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181123 71095 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 591 11 1 6 5.1 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)S(=O)(=O)Cc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
10600702 148114 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL383526 148114 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
10600702 148114 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL383526 148114 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
9868878 103316 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 460 14 4 9 -0.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCC(N)=O 10.1016/j.bmcl.2008.03.059
CHEMBL262884 103316 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 460 14 4 9 -0.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCC(N)=O 10.1016/j.bmcl.2008.03.059
11306502 70416 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180094 70416 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
22888395 70679 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 513 10 1 4 5.2 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180540 70679 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 513 10 1 4 5.2 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
156021942 185002 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4649860 185002 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
16113248 85939 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 560 11 3 5 5.6 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
CHEMBL2113328 85939 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 560 11 3 5 5.6 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
23730342 96677 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 511 13 4 10 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCc1cccc(O)c1 10.1021/jm7010595
CHEMBL237916 96677 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 511 13 4 10 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCc1cccc(O)c1 10.1021/jm7010595
145958487 168963 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc(F)c21 10.1021/acs.jmedchem.8b00322
CHEMBL4162545 168963 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc(F)c21 10.1021/acs.jmedchem.8b00322
156010733 183859 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633062 183859 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156013130 184281 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639514 184281 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156016840 184410 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 621 7 3 7 3.4 Cc1nc(-c2cccc(C(F)(F)F)c2)sc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4641215 184410 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 621 7 3 7 3.4 Cc1nc(-c2cccc(C(F)(F)F)c2)sc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
156021942 185002 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4649860 185002 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44570920 190712 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 413 4 1 4 2.5 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL481408 190712 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 413 4 1 4 2.5 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
44571005 190826 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 431 4 1 5 2.6 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CCCNCC3)cc2)o1 10.1016/j.bmcl.2008.12.042
CHEMBL482204 190826 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 431 4 1 5 2.6 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CCCNCC3)cc2)o1 10.1016/j.bmcl.2008.12.042
11539144 95668 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 425 5 2 5 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2ccccc2c1 10.6019/CHEMBL2364335
CHEMBL2364356 95668 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 425 5 2 5 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2ccccc2c1 10.6019/CHEMBL2364335
69197315 95684 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1cc(F)c(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364372 95684 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1cc(F)c(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
11683663 95710 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccoc2)cc1 10.6019/CHEMBL2364335
CHEMBL2364398 95710 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccoc2)cc1 10.6019/CHEMBL2364335
11583902 95751 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 484 6 2 6 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)cc1F 10.6019/CHEMBL2364335
CHEMBL2364437 95751 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 484 6 2 6 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)cc1F 10.6019/CHEMBL2364335
69198030 95756 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 479 5 2 5 5.2 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)cc3Cl)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364442 95756 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 479 5 2 5 5.2 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)cc3Cl)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69197149 95768 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)c(C)c1 10.6019/CHEMBL2364335
CHEMBL2364454 95768 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)c(C)c1 10.6019/CHEMBL2364335
69196669 95793 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 456 6 2 7 3.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)nc1 10.6019/CHEMBL2364335
CHEMBL2364478 95793 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 456 6 2 7 3.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)nc1 10.6019/CHEMBL2364335
10032659 18823 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 587 11 4 8 -0.5 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@H](CO)NC(=O)CN)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL1183505 18823 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 587 11 4 8 -0.5 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@H](CO)NC(=O)CN)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL301259 18823 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 587 11 4 8 -0.5 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@H](CO)NC(=O)CN)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
44450137 103076 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 465 12 3 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)Nc1ccccc1 10.1016/j.bmcl.2008.03.059
CHEMBL261234 103076 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 465 12 3 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)Nc1ccccc1 10.1016/j.bmcl.2008.03.059
127046472 146472 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1021/acs.jmedchem.1c02191
CHEMBL3798056 146472 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1021/acs.jmedchem.1c02191
127046472 146472 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayInverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798056 146472 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayInverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
145988286 173985 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 542 6 1 6 5.4 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-n5nccn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4291718 173985 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 542 6 1 6 5.4 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-n5nccn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL3578007 218540 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm501702q
CHEMBL61663 222618 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/s0960-894x(01)00324-9
24180592 103788 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
CHEMBL266647 103788 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
162663868 188767 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 672 14 3 9 3.8 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4780408 188767 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 672 14 3 9 3.8 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
145986080 173231 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 489 5 1 3 6.2 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(C)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4277793 173231 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 489 5 1 3 6.2 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(C)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
168274297 197358 0 None - 1 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 299 6 1 1 5.3 CCCCCCCc1cc(=O)c2cc(C(C)(C)C)ccc2[nH]1 10.1021/acs.jmedchem.1c02191
CHEMBL5180310 197358 0 None - 1 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 299 6 1 1 5.3 CCCCCCCc1cc(=O)c2cc(C(C)(C)C)ccc2[nH]1 10.1021/acs.jmedchem.1c02191
127047523 146841 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 859 20 7 9 6.0 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3800422 146841 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 859 20 7 9 6.0 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)O)cc1 10.1016/j.bmcl.2016.04.003
44434118 154957 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 467 14 3 9 0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCCNS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL393570 154957 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 467 14 3 9 0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCCNS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
44446187 101396 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252255 101396 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
145959787 169064 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 169064 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
155557019 181366 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4556887 181366 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
56926893 75838 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 10.1021/jm2007062
CHEMBL1923637 75838 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 10.1021/jm2007062
44437963 208871 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 452 6 1 3 4.5 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c(Br)cccc21 10.1016/j.bmc.2007.01.057
CHEMBL608826 208871 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 452 6 1 3 4.5 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c(Br)cccc21 10.1016/j.bmc.2007.01.057
44437963 208871 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 452 6 1 3 4.5 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c(Br)cccc21 10.1016/j.bmc.2007.01.057
CHEMBL608826 208871 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 452 6 1 3 4.5 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c(Br)cccc21 10.1016/j.bmc.2007.01.057
44579881 193615 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1ccccc1Cl 10.1016/j.bmcl.2008.07.120
CHEMBL489402 193615 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1ccccc1Cl 10.1016/j.bmcl.2008.07.120
24180646 154961 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1021/jm701137s
CHEMBL393576 154961 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1021/jm701137s
24180646 154961 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
CHEMBL393576 154961 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
145959787 169064 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 169064 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
46882520 12628 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 430 5 2 4 3.8 Cc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1Cl 10.1016/j.bmcl.2009.09.027
CHEMBL1079311 12628 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 430 5 2 4 3.8 Cc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1Cl 10.1016/j.bmcl.2009.09.027
46882458 12750 0 None -31 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 438 8 2 4 4.2 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1080046 12750 0 None -31 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 438 8 2 4 4.2 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL3578016 218546 0 None -15 2 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
59007057 95667 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 6 2.8 COc1ccc(NS(=O)(=O)c2ccc(N3CCCC3=O)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364355 95667 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 6 2.8 COc1ccc(NS(=O)(=O)c2ccc(N3CCCC3=O)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11597905 95721 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 6 2 5 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(C)cc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364409 95721 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 6 2 5 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(C)cc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69198135 95752 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 484 6 2 6 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)c(F)c1 10.6019/CHEMBL2364335
CHEMBL2364438 95752 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 484 6 2 6 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)c(F)c1 10.6019/CHEMBL2364335
11711997 95769 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 446 5 2 7 2.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2c(c1)OCCN2C 10.6019/CHEMBL2364335
CHEMBL2364455 95769 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 446 5 2 7 2.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2c(c1)OCCN2C 10.6019/CHEMBL2364335
44452778 166557 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 499 6 2 7 3.5 C[C@H]1CN(c2ccc(C(=O)N(C)C)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
CHEMBL410527 166557 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 499 6 2 7 3.5 C[C@H]1CN(c2ccc(C(=O)N(C)C)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
10437444 119658 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 546 11 2 4 3.8 CNC(=O)[C@@H](Cc1ccc(F)cc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL330989 119658 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 546 11 2 4 3.8 CNC(=O)[C@@H](Cc1ccc(F)cc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
24969603 75829 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 520 3 3 5 2.4 Cc1ccc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NCCOc3ccccc3CCCNC2=O)cc1 10.1021/jm2007062
CHEMBL1923627 75829 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 520 3 3 5 2.4 Cc1ccc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NCCOc3ccccc3CCCNC2=O)cc1 10.1021/jm2007062
162649450 186833 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 725 14 3 10 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C2CCN(c3oc(C)nc3C#N)CC2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4747770 186833 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 725 14 3 10 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C2CCN(c3oc(C)nc3C#N)CC2)cc1 10.1021/acs.jmedchem.9b02122
156013130 184281 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639514 184281 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44450100 167434 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 511 14 4 10 0.6 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1cccc(C(=O)NCCO)c1 10.1016/j.bmcl.2008.03.059
CHEMBL411330 167434 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 511 14 4 10 0.6 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1cccc(C(=O)NCCO)c1 10.1016/j.bmcl.2008.03.059
44411720 17079 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161826 17079 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
44411902 17083 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161831 17083 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
44411720 17079 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161826 17079 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
44411902 17083 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161831 17083 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
162656896 187639 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 669 14 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2cccs2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4757313 187639 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 669 14 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2cccs2)cc1 10.1021/acs.jmedchem.9b02122
44436883 152931 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 604 11 6 7 3.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2c[nH]c3ccccc23)cc1 10.1021/jm0704550
CHEMBL391980 152931 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 604 11 6 7 3.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2c[nH]c3ccccc23)cc1 10.1021/jm0704550
156010733 183859 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633062 183859 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
10745674 174733 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 572 13 3 5 3.5 C[C@@H](O)CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL431668 174733 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 572 13 3 5 3.5 C[C@@H](O)CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
44579776 200030 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 352 7 1 3 3.5 Cc1cccc(CN(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
CHEMBL523795 200030 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 352 7 1 3 3.5 Cc1cccc(CN(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
127048061 146514 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 903 24 7 11 5.9 COC(=O)[C@H](CC(C)C)NC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798337 146514 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 903 24 7 11 5.9 COC(=O)[C@H](CC(C)C)NC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
23730340 96516 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 504 15 4 10 0.4 CC(=O)NCCCCNC(=O)OCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1021/jm7010595
CHEMBL237700 96516 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 504 15 4 10 0.4 CC(=O)NCCCCNC(=O)OCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1021/jm7010595
56926175 75788 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923504 75788 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
145992835 173613 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cncnc4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4285075 173613 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cncnc4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
56925343 75841 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 550 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cccc3c2O[C@H](CC3)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923640 75841 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 550 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cccc3c2O[C@H](CC3)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
145986870 173919 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 505 6 1 4 5.9 COc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(OC)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4290627 173919 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 505 6 1 4 5.9 COc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(OC)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
44434054 96079 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2cccc(NS(C)(=O)=O)c2)n1 10.1016/j.bmcl.2007.07.099
CHEMBL236857 96079 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2cccc(NS(C)(=O)=O)c2)n1 10.1016/j.bmcl.2007.07.099
44446178 161902 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL402023 161902 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL3578016 218546 0 None -15 2 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
162648837 186617 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 706 15 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4745116 186617 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 706 15 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
44391024 71059 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 527 11 1 4 5.2 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)Cc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180992 71059 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 527 11 1 4 5.2 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)Cc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
10745674 174733 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 572 13 3 5 3.5 C[C@@H](O)CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL431668 174733 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 572 13 3 5 3.5 C[C@@H](O)CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
44391021 26225 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 569 12 1 5 5.3 CC(=O)C(C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C)c1ccccc1 10.1016/j.bmcl.2005.02.040
CHEMBL129637 26225 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 569 12 1 5 5.3 CC(=O)C(C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C)c1ccccc1 10.1016/j.bmcl.2005.02.040
CHEMBL2170696 216135 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1csc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1csc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
23730343 96678 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 475 12 3 10 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NC[C@H]1CCCO1 10.1021/jm7010595
CHEMBL237917 96678 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 475 12 3 10 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NC[C@H]1CCCO1 10.1021/jm7010595
22888359 70690 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 520 10 1 6 4.8 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C#N)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180591 70690 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 520 10 1 6 4.8 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C#N)C(C)C 10.1016/j.bmcl.2005.02.040
16114514 85933 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCCNC1 10.1021/jm0704550
CHEMBL2113322 85933 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCCNC1 10.1021/jm0704550
44579843 191532 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL485092 191532 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
44579643 193550 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 338 7 1 3 3.2 CC(Oc1ccccc1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL488971 193550 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 338 7 1 3 3.2 CC(Oc1ccccc1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44579822 199303 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1cccc(CN(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL520953 199303 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1cccc(CN(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2Cl)c1 10.1016/j.bmcl.2008.07.120
44579755 193722 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 352 8 1 3 3.6 CCC(Oc1ccccc1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL490186 193722 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 352 8 1 3 3.6 CCC(Oc1ccccc1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44580032 193613 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 363 7 1 4 3.3 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(CC#N)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL489398 193613 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 363 7 1 4 3.3 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(CC#N)cc1 10.1016/j.bmcl.2008.07.120
145991945 173594 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 615 6 1 4 7.8 CCN(C(=O)N[C@@H](C)c1ccc(C#CC2CC2)c(Cl)c1Cl)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4284715 173594 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 615 6 1 4 7.8 CCN(C(=O)N[C@@H](C)c1ccc(C#CC2CC2)c(Cl)c1Cl)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1 10.1021/acs.jmedchem.8b00794
145992253 173707 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 595 6 1 6 6.4 COC(=O)c1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4286849 173707 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 595 6 1 6 6.4 COC(=O)c1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL2170702 216141 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
145993313 173671 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 577 7 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3cccc(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4286101 173671 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 577 7 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3cccc(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
16114008 91621 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 536 11 3 6 4.7 COc1ccccc1Cn1c(CCc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL223532 91621 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 536 11 3 6 4.7 COc1ccccc1Cn1c(CCc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL501261 220914 23 None - 1 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.8b01644
9848305 152230 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccc(NS(C)(=O)=O)cc2)n1 10.1016/j.bmcl.2007.07.099
CHEMBL391429 152230 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccc(NS(C)(=O)=O)cc2)n1 10.1016/j.bmcl.2007.07.099
44434050 152228 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL391428 152228 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL3578015 218545 0 None -33 2 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
CHEMBL369482 218942 0 None - 0 Rat 8.0 pED50 = 8 Functional
In vitro effective dose was measured for the growth hormone release in rat pituitary cellsIn vitro effective dose was measured for the growth hormone release in rat pituitary cells
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cn1ccnc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/S0960-894X(01)80239-0
44269087 105003 0 None - 1 Rat 6.7 pED50 = 6.7 Functional
In vitro effective dose was measured for the growth hormone release in rat pituitary cellsIn vitro effective dose was measured for the growth hormone release in rat pituitary cells
ChEMBL 553 10 4 7 3.2 CC(C)(NCCCO)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=O 10.1016/S0960-894X(01)80239-0
CHEMBL274341 105003 0 None - 1 Rat 6.7 pED50 = 6.7 Functional
In vitro effective dose was measured for the growth hormone release in rat pituitary cellsIn vitro effective dose was measured for the growth hormone release in rat pituitary cells
ChEMBL 553 10 4 7 3.2 CC(C)(NCCCO)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=O 10.1016/S0960-894X(01)80239-0
70691550 79975 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 572 8 2 5 5.1 Cc1cc(F)ccc1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
CHEMBL2011825 79975 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 572 8 2 5 5.1 Cc1cc(F)ccc1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
16114292 103709 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL266063 103709 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL509976 222359 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Agonist activity at human ghrelin receptor Met5:05Ala(Met213) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Met5:05Ala(Met213) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
25260901 120257 1 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL 577 5 2 9 3.6 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/acs.jmedchem.1c02191
CHEMBL3319405 120257 1 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL 577 5 2 9 3.6 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/acs.jmedchem.1c02191
71456897 88625 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 513 5 2 3 5.7 CCN1CCC(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164507 88625 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 513 5 2 3 5.7 CCN1CCC(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
70691551 79976 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 568 8 2 5 5.3 Cc1cccc(C)c1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
CHEMBL2011826 79976 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 568 8 2 5 5.3 Cc1cccc(C)c1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
25261382 120218 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Partial agonist activity at GHS-R1a (unknown origin)Partial agonist activity at GHS-R1a (unknown origin)
ChEMBL 535 7 2 8 3.3 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/acs.jmedchem.1c02191
CHEMBL3319215 120218 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Partial agonist activity at GHS-R1a (unknown origin)Partial agonist activity at GHS-R1a (unknown origin)
ChEMBL 535 7 2 8 3.3 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/acs.jmedchem.1c02191
11431274 84119 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 467 9 3 8 3.8 CC(C)=CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL208424 84119 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 467 9 3 8 3.8 CC(C)=CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11577349 72005 1 None - 1 Human 8.0 pIC50 = 8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 529 9 1 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCN(C)C2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL182655 72005 1 None - 1 Human 8.0 pIC50 = 8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 529 9 1 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCN(C)C2=O)cc1 10.1016/j.bmcl.2004.06.060
11351838 84425 0 None - 1 Human 8.0 pIC50 = 8 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 468 8 4 6 4.9 CC(NC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1)c1ccccc1 10.1021/jm060461g
CHEMBL208842 84425 0 None - 1 Human 8.0 pIC50 = 8 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 468 8 4 6 4.9 CC(NC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1)c1ccccc1 10.1021/jm060461g
11712151 82768 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 453 9 3 7 4.8 CC(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL205470 82768 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 453 9 3 7 4.8 CC(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
11713497 130015 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 531 9 1 6 6.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)c(C)c1 10.1016/j.bmcl.2004.11.075
CHEMBL361349 130015 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 531 9 1 6 6.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)c(C)c1 10.1016/j.bmcl.2004.11.075
44409757 148102 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 506 8 3 8 4.1 CN(Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL383454 148102 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 506 8 3 8 4.1 CN(Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2006.01.012
127046807 146718 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799671 146718 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
3676358 12306 4 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 409 3 1 2 4.4 O=C(c1ccc(-c2ccccc2)cc1)N1CCN(C(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/j.bmcl.2010.01.043
CHEMBL1076586 12306 4 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 409 3 1 2 4.4 O=C(c1ccc(-c2ccccc2)cc1)N1CCN(C(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/j.bmcl.2010.01.043
122182047 128780 0 None -67 2 Rat 7.0 pIC50 = 7 Functional
Antagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assayAntagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assay
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593636 128780 0 None -67 2 Rat 7.0 pIC50 = 7 Functional
Antagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assayAntagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assay
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
122178603 128117 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 590 11 2 6 6.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(Cl)nc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581036 128117 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 590 11 2 6 6.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(Cl)nc2)cc1 10.1016/j.bmcl.2014.11.031
11649248 73444 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 515 9 1 5 7.2 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL185399 73444 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 515 9 1 5 7.2 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCCO2)cc1 10.1016/j.bmcl.2004.06.060
44395020 130810 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 507 9 1 5 6.1 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL363021 130810 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 507 9 1 5 6.1 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)CC1 10.1016/j.bmcl.2004.06.060
44389262 128810 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 479 6 2 4 6.1 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccccc1 10.1016/j.bmcl.2004.11.075
CHEMBL359506 128810 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 479 6 2 4 6.1 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccccc1 10.1016/j.bmcl.2004.11.075
145993628 174170 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 483 4 1 2 6.1 C#Cc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(C)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4295148 174170 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 483 4 1 2 6.1 C#Cc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(C)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
11211892 86991 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 405 8 3 6 4.0 CC(C)CC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
CHEMBL213703 86991 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 405 8 3 6 4.0 CC(C)CC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
122178611 128126 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 572 11 3 7 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2O)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581044 128126 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 572 11 3 7 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2O)cc1 10.1016/j.bmcl.2014.11.031
11846624 84691 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 490 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(C1CCCC1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
CHEMBL209443 84691 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 490 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(C1CCCC1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
11846463 146020 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 422 5 2 8 2.7 CCc1nc(N)nc(N)c1-c1ccc2c(c1)ncn2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
CHEMBL378909 146020 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 422 5 2 8 2.7 CCc1nc(N)nc(N)c1-c1ccc2c(c1)ncn2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
11430392 83499 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 431 6 3 7 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Cl)c1 10.1021/jm0510934
CHEMBL206588 83499 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 431 6 3 7 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Cl)c1 10.1021/jm0510934
57797614 79967 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 558 8 2 5 4.8 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(F)cc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011817 79967 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 558 8 2 5 4.8 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(F)cc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
44409801 83508 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 5 3 7 3.6 CC(C)(C)c1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206638 83508 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 5 3 7 3.6 CC(C)(C)c1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11523411 82330 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 363 6 4 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)O)cc2)cc1 10.1021/jm0510934
CHEMBL204511 82330 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 363 6 4 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)O)cc2)cc1 10.1021/jm0510934
11537800 82342 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 361 6 3 6 3.7 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)=O)cc2)cc1 10.1021/jm0510934
CHEMBL204564 82342 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 361 6 3 6 3.7 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)=O)cc2)cc1 10.1021/jm0510934
71453392 88622 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 5 2 4 4.2 CN(C)[C@H]1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)C1 10.1016/j.bmc.2012.07.018
CHEMBL2164504 88622 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 5 2 4 4.2 CN(C)[C@H]1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)C1 10.1016/j.bmc.2012.07.018
71456910 88676 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 480 5 2 4 3.6 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164823 88676 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 480 5 2 4 3.6 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
71460578 88683 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)ccc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164830 88683 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)ccc32)CC1 10.1016/j.bmc.2012.07.018
122178612 128127 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 572 11 2 6 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc[n+]2[O-])cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581045 128127 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 572 11 2 6 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc[n+]2[O-])cc1 10.1016/j.bmcl.2014.11.031
CHEMBL507636 221212 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H]1CCCN1C(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1074/jbc.m609796200
56942387 146440 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 579 13 4 7 4.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797857 146440 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 579 13 4 7 4.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
145991822 173738 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 6.8 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)NCc3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4287267 173738 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 6.8 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)NCc3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
11676995 72936 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 461 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCOC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL184258 72936 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 461 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCOC)cc1 10.1016/j.bmcl.2004.06.060
127048038 146750 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 551 11 4 7 4.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799862 146750 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 551 11 4 7 4.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
71458746 88612 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1ccc2c(c1Cl)C(NC(=O)CN1CCN(C)CC1)(c1ccc(Cl)cc1)C(=O)N2 10.1016/j.bmc.2012.07.018
CHEMBL2164493 88612 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1ccc2c(c1Cl)C(NC(=O)CN1CCN(C)CC1)(c1ccc(Cl)cc1)C(=O)N2 10.1016/j.bmc.2012.07.018
145992142 173550 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 475 4 2 3 5.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(O)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4283858 173550 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 475 4 2 3 5.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(O)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
71460565 88614 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1cccc(Cl)c1 10.1016/j.bmc.2012.07.018
CHEMBL2164495 88614 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1cccc(Cl)c1 10.1016/j.bmc.2012.07.018
11538533 81776 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
CHEMBL203280 81776 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
46880462 13039 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)[C@@H](C)C3)cc2)c1 10.1016/j.bmcl.2010.01.043
CHEMBL1081648 13039 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)[C@@H](C)C3)cc2)c1 10.1016/j.bmcl.2010.01.043
70693641 79978 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 538 8 2 5 4.4 O=C1CN([C@@H](C(=O)NC2CCN(Cc3ccccc3)CC2)C2CC2)C(=O)c2cc(Oc3ccccc3)ccc2N1 10.1016/j.bmcl.2012.01.014
CHEMBL2011828 79978 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 538 8 2 5 4.4 O=C1CN([C@@H](C(=O)NC2CCN(Cc3ccccc3)CC2)C2CC2)C(=O)c2cc(Oc3ccccc3)ccc2N1 10.1016/j.bmcl.2012.01.014
44409756 83542 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 492 8 4 8 4.1 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccc(F)cc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206820 83542 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 492 8 4 8 4.1 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccc(F)cc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
46865987 14369 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 442 3 1 3 4.4 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3)c(F)c2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1087908 14369 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 442 3 1 3 4.4 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3)c(F)c2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
46880772 12683 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1079624 12683 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
11538534 81789 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
CHEMBL203373 81789 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
145986870 173919 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 505 6 1 4 5.9 COc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(OC)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4290627 173919 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 505 6 1 4 5.9 COc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(OC)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
127046806 146711 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 638 13 4 7 5.4 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799604 146711 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 638 13 4 7 5.4 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
122178613 128128 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 625 12 2 7 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(N3CCCC3)cn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581046 128128 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 625 12 2 7 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(N3CCCC3)cn2)cc1 10.1016/j.bmcl.2014.11.031
145981196 173315 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 627 5 1 6 7.1 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)N[C@@H](C)c4ccc(-c5cnccn5)c(Cl)c4Cl)CC3)C2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4279344 173315 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 627 5 1 6 7.1 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)N[C@@H](C)c4ccc(-c5cnccn5)c(Cl)c4Cl)CC3)C2)ncn1 10.1021/acs.jmedchem.8b00794
46880814 13149 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 413 3 2 3 3.5 C[C@H]1CN(C(=O)c2ccc(-c3cn[nH]c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1082190 13149 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 413 3 2 3 3.5 C[C@H]1CN(C(=O)c2ccc(-c3cn[nH]c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
122178616 128130 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc3ccccc3cn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581048 128130 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc3ccccc3cn2)cc1 10.1016/j.bmcl.2014.11.031
145986461 173992 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4291926 173992 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
71451551 88626 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 460 5 2 4 3.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(C)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164508 88626 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 460 5 2 4 3.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(C)cc32)CC1 10.1016/j.bmc.2012.07.018
46880727 12917 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 458 3 1 3 4.9 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3Cl)nc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080939 12917 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 458 3 1 3 4.9 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3Cl)nc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
122182190 128787 0 None -8 2 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assayAntagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assay
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
CHEMBL3593815 128787 0 None -8 2 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assayAntagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assay
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
44409840 83117 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 500 7 3 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN3CCc4ccccc43)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205896 83117 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 500 7 3 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN3CCc4ccccc43)cc2)cc1 10.1016/j.bmcl.2006.01.012
127047362 146497 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 590 11 5 7 4.7 COc1ccc(Cn2c([C@H](N)Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798204 146497 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 590 11 5 7 4.7 COc1ccc(Cn2c([C@H](N)Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
145989916 173525 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 491 5 2 4 5.6 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(O)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4283454 173525 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 491 5 2 4 5.6 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(O)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
127048038 146750 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 551 11 4 7 4.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799862 146750 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 551 11 4 7 4.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
46880673 12877 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 507 4 1 3 5.7 C[C@H]1CN(C(=O)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080755 12877 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 507 4 1 3 5.7 C[C@H]1CN(C(=O)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
11455251 168093 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 523 8 3 7 5.0 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3Br)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL412362 168093 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 523 8 3 7 5.0 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3Br)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
44409611 81462 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 463 6 3 7 4.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CC4CCC3C4)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203019 81462 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 463 6 3 7 4.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CC4CCC3C4)cc2)cc1 10.1016/j.bmcl.2006.01.012
11221946 147624 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm0510934
CHEMBL381942 147624 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm0510934
44409839 83033 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 412 7 4 8 2.0 CNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205847 83033 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 412 7 4 8 2.0 CNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
71460576 88680 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3c(Cl)cc(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164828 88680 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3c(Cl)cc(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL509976 222359 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Agonist activity at human ghrelin receptor Ser5:09Ala(Ser217) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Ser5:09Ala(Ser217) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
11692087 69766 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178610 69766 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.11.075
44409758 82749 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 411 6 3 7 3.4 CC(C)c1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205374 82749 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 411 6 3 7 3.4 CC(C)c1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409661 82771 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 423 6 3 7 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205484 82771 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 423 6 3 7 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
46880724 13030 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 437 3 1 2 5.1 Cc1cc(-c2ccccc2)ccc1C(=O)N1CCN(C(=O)c2ccc3cc[nH]c3c2)[C@@H](C)C1 10.1016/j.bmcl.2010.01.043
CHEMBL1081611 13030 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 437 3 1 2 5.1 Cc1cc(-c2ccccc2)ccc1C(=O)N1CCN(C(=O)c2ccc3cc[nH]c3c2)[C@@H](C)C1 10.1016/j.bmcl.2010.01.043
71455105 88679 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 432 4 2 4 2.6 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)ccc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164827 88679 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 432 4 2 4 2.6 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)ccc32)CC1 10.1016/j.bmc.2012.07.018
11221946 147624 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm060461g
CHEMBL381942 147624 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm060461g
44410003 82956 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 468 10 4 8 3.5 CC(C)CCNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205794 82956 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 468 10 4 8 3.5 CC(C)CCNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
46880811 12770 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3cccnc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080162 12770 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3cccnc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
70687379 79973 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 570 9 2 6 4.7 COc1cccc(Oc2ccc3c(c2)C(=O)N([C@@H](C(=O)NC2CCN(Cc4ccccc4)CC2)C(C)C)CC(=O)N3)c1 10.1016/j.bmcl.2012.01.014
CHEMBL2011823 79973 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 570 9 2 6 4.7 COc1cccc(Oc2ccc3c(c2)C(=O)N([C@@H](C(=O)NC2CCN(Cc4ccccc4)CC2)C(C)C)CC(=O)N3)c1 10.1016/j.bmcl.2012.01.014
44394974 73786 1 None - 1 Human 6.8 pIC50 = 6.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 515 9 1 5 7.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCOCC2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL186974 73786 1 None - 1 Human 6.8 pIC50 = 6.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 515 9 1 5 7.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCOCC2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL3586019 218580 6 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by inositol phosphate turnover assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by inositol phosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CCCNC(=N)N)C(N)=O 10.1016/j.bmcl.2015.04.040
46880567 13159 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3cccc(F)c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1082210 13159 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3cccc(F)c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
71460564 88611 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 488 4 2 4 3.9 CN1CCN(CC(=O)NC2(c3ccc(C(C)(C)C)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164492 88611 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 488 4 2 4 3.9 CN1CCN(CC(=O)NC2(c3ccc(C(C)(C)C)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
145992854 173645 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 7.0 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)C2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4285747 173645 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 7.0 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)C2)ncn1 10.1021/acs.jmedchem.8b00794
44394833 133603 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 542 9 1 5 6.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2C(=O)CCC2(C)C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL365460 133603 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 542 9 1 5 6.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2C(=O)CCC2(C)C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL509976 222359 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Agonist activity at human ghrelin receptor Asn7:02Ala(Asn305) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Asn7:02Ala(Asn305) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
CHEMBL509976 222359 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Agonist activity at human wild type ghrelin receptor expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human wild type ghrelin receptor expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
CHEMBL509976 222359 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
127047654 146755 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799883 146755 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
145993758 174095 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 490 5 2 4 5.4 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(N)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4294024 174095 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 490 5 2 4 5.4 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(N)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
145993528 174097 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 561 5 1 4 6.6 C#Cc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4294083 174097 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 561 5 1 4 6.6 C#Cc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL444131 220708 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None NC(=O)CNC(=O)CNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1c[nH]c2ccccc12 10.1074/jbc.m609796200
11476589 82763 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(CNc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205451 82763 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(CNc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
11329138 71234 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilizationAntagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilization
ChEMBL 481 9 1 5 5.1 CCN(CC)c1ccc(NC(=O)C2(N(C)C(=O)OCC(C)C)CCc3cccc(OC)c3C2)cc1 10.1016/j.bmcl.2012.01.014
CHEMBL181350 71234 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilizationAntagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilization
ChEMBL 481 9 1 5 5.1 CCN(CC)c1ccc(NC(=O)C2(N(C)C(=O)OCC(C)C)CCc3cccc(OC)c3C2)cc1 10.1016/j.bmcl.2012.01.014
70681022 79982 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 568 8 2 5 5.4 CC(C)[C@H](C(=O)N1CCC(NC(C)(C)c2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011833 79982 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 568 8 2 5 5.4 CC(C)[C@H](C(=O)N1CCC(NC(C)(C)c2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL509976 222359 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human ghrelin receptor Ile4:20Ala(Ile178) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Ile4:20Ala(Ile178) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
122178611 128126 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 572 11 3 7 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2O)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581044 128126 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 572 11 3 7 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2O)cc1 10.1016/j.bmcl.2014.11.031
46880675 12915 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3)cc2F)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080927 12915 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3)cc2F)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
11612155 147787 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3csc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL382375 147787 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3csc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
328912 69350 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 505 5 1 4 7.0 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1CC1c2ccccc2CCN1C 10.1016/j.bmcl.2004.11.075
CHEMBL178266 69350 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 505 5 1 4 7.0 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1CC1c2ccccc2CCN1C 10.1016/j.bmcl.2004.11.075
70685218 79970 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 574 8 2 5 5.3 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3cccc(Cl)c3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011820 79970 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 574 8 2 5 5.3 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3cccc(Cl)c3)cc2C1=O 10.1016/j.bmcl.2012.01.014
145981794 173475 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 567 6 1 5 6.6 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4282394 173475 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 567 6 1 5 6.6 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
11649239 73114 1 None - 1 Human 7.8 pIC50 = 7.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 514 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL185057 73114 1 None - 1 Human 7.8 pIC50 = 7.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 514 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL501261 220914 23 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)CCCNC(=N)N)C(N)=O 10.1074/jbc.m609796200
1744826 69772 17 None - 1 Human 6.8 pIC50 = 6.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL178668 69772 17 None - 1 Human 6.8 pIC50 = 6.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.06.060
11282247 172705 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL425048 172705 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
11282247 172705 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL425048 172705 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
1744826 69772 17 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178668 69772 17 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44409831 82473 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 503 6 3 9 3.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3COc4ccccc4O3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204776 82473 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 503 6 3 9 3.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3COc4ccccc4O3)cc2)cc1 10.1016/j.bmcl.2006.01.012
145979268 173443 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 607 8 1 5 7.4 COc1ccc([C@H](CC2CC2)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4281647 173443 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 607 8 1 5 7.4 COc1ccc([C@H](CC2CC2)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
44409678 147995 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 490 9 3 9 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3cccnc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL382853 147995 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 490 9 3 9 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3cccnc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11349789 85548 1 None - 1 Human 6.7 pIC50 = 6.7 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 389 7 3 6 3.4 Nc1nc(N)c(-c2ccc(NC(=O)C3CC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL211265 85548 1 None - 1 Human 6.7 pIC50 = 6.7 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 389 7 3 6 3.4 Nc1nc(N)c(-c2ccc(NC(=O)C3CC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
11692087 69766 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL178610 69766 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.06.060
11677781 131836 1 None - 1 Human 7.7 pIC50 = 7.7 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 502 9 1 5 5.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN(C)C(C)=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL364430 131836 1 None - 1 Human 7.7 pIC50 = 7.7 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 502 9 1 5 5.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN(C)C(C)=O)cc1 10.1016/j.bmcl.2004.06.060
11538533 81776 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm060461g
CHEMBL203280 81776 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm060461g
11154823 82804 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 436 8 3 7 4.5 N#Cc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL205660 82804 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 436 8 3 7 4.5 N#Cc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
56942244 131975 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645259 131975 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
44409994 82957 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 409 6 3 7 3.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205796 82957 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 409 6 3 7 3.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44576247 221001 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inverse agonist activity at human ghrelin receptor Phe5:12Ala(Phe220) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Phe5:12Ala(Phe220) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 221001 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inverse agonist activity at human ghrelin receptor Phe5:12Ala(Phe220) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Phe5:12Ala(Phe220) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
44395002 72960 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 534 9 1 5 5.6 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL184368 72960 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 534 9 1 5 5.6 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)CC1 10.1016/j.bmcl.2004.06.060
11646276 82709 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
CHEMBL205136 82709 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
127046807 146718 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799671 146718 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
16113695 143805 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL374643 143805 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
145987684 174056 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 615 6 1 4 7.8 CC[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4293331 174056 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 615 6 1 4 7.8 CC[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
122178602 128116 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2Br)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581035 128116 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2Br)cc1 10.1016/j.bmcl.2014.11.031
70681020 79979 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011829 79979 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
56942098 131971 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645255 131971 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
56942242 131973 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645257 131973 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 10.1016/j.bmcl.2016.04.003
127046956 146735 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 631 12 3 7 5.5 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799776 146735 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 631 12 3 7 5.5 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2016.04.003
66788278 131970 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645254 131970 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
127046956 146735 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 631 12 3 7 5.5 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799776 146735 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 631 12 3 7 5.5 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2016.04.003
57797640 80001 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 510 9 1 3 7.1 CC(C)[C@H](C[C@H]1CC[C@@H](NCC2CC2)CC1)N1CCCc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011892 80001 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 510 9 1 3 7.1 CC(C)[C@H](C[C@H]1CC[C@@H](NCC2CC2)CC1)N1CCCc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
46880628 12804 0 None 4 2 Rat 8.7 pIC50 = 8.7 Functional
Inhibition of rat GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayInhibition of rat GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080389 12804 0 None 4 2 Rat 8.7 pIC50 = 8.7 Functional
Inhibition of rat GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayInhibition of rat GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
122178606 128120 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(F)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581039 128120 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(F)n2)cc1 10.1016/j.bmcl.2014.11.031
46880629 12830 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 457 3 1 2 5.5 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3Cl)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080556 12830 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 457 3 1 2 5.5 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3Cl)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
122178606 128120 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(F)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581039 128120 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(F)n2)cc1 10.1016/j.bmcl.2014.11.031
70681021 79981 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 554 8 2 5 5.2 CC(C)[C@H](C(=O)N1CCC(N[C@H](C)c2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011832 79981 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 554 8 2 5 5.2 CC(C)[C@H](C(=O)N1CCC(N[C@H](C)c2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
70691552 79983 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 560 8 2 5 5.4 CC(C)[C@H](C(=O)N1CCC(N[C@H](C)C2CCCCC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011834 79983 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 560 8 2 5 5.4 CC(C)[C@H](C(=O)N1CCC(N[C@H](C)C2CCCCC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
44576247 221001 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inverse agonist activity at human ghrelin receptor Ser4:16Ala(Ser174) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ser4:16Ala(Ser174) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 221001 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inverse agonist activity at human ghrelin receptor Ser4:16Ala(Ser174) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ser4:16Ala(Ser174) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
122178607 128122 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 592 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncc(F)cc2F)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581040 128122 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 592 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncc(F)cc2F)cc1 10.1016/j.bmcl.2014.11.031
46880631 12907 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 437 3 1 2 5.1 Cc1ccccc1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1 10.1016/j.bmcl.2010.01.043
CHEMBL1080907 12907 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 437 3 1 2 5.1 Cc1ccccc1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1 10.1016/j.bmcl.2010.01.043
46880726 12916 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3)nc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080938 12916 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3)nc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
70689441 80000 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 525 9 2 4 6.1 CC(C)[C@H](C[C@H]1CC[C@@H](NCC2CC2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011891 80000 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 525 9 2 4 6.1 CC(C)[C@H](C[C@H]1CC[C@@H](NCC2CC2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
145988582 174070 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 555 4 1 2 7.4 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C#C[Si](C)(C)C)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4293608 174070 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 555 4 1 2 7.4 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C#C[Si](C)(C)C)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
122178610 128125 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(N)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581043 128125 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(N)n2)cc1 10.1016/j.bmcl.2014.11.031
44409666 82662 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 437 6 3 7 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204897 82662 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 437 6 3 7 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44576247 221001 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inverse agonist activity at human ghrelin receptor Ser3:08Ala(Ser123) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ser3:08Ala(Ser123) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 221001 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inverse agonist activity at human ghrelin receptor Ser3:08Ala(Ser123) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ser3:08Ala(Ser123) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL500703 220899 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCNC(=N)N)C(N)=O 10.1074/jbc.m609796200
44409802 83519 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 9 3 7 4.1 CCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206687 83519 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 9 3 7 4.1 CCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122178613 128128 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 625 12 2 7 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(N3CCCC3)cn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581046 128128 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 625 12 2 7 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(N3CCCC3)cn2)cc1 10.1016/j.bmcl.2014.11.031
71458747 88613 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2012.07.018
CHEMBL2164494 88613 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2012.07.018
56942244 131975 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645259 131975 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
11537683 82302 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 354 5 3 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccnc(Cl)c2)cc1 10.1021/jm0510934
CHEMBL204352 82302 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 354 5 3 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccnc(Cl)c2)cc1 10.1021/jm0510934
71449740 88615 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 480 4 2 4 3.5 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2012.07.018
CHEMBL2164497 88615 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 480 4 2 4 3.5 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2012.07.018
122178601 128115 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cncc(Br)c2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581034 128115 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cncc(Br)c2)cc1 10.1016/j.bmcl.2014.11.031
11337482 83415 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
CHEMBL206399 83415 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
122178614 128129 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 660 13 2 7 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2C(=O)c2ccccc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581047 128129 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 660 13 2 7 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2C(=O)c2ccccc2)cc1 10.1016/j.bmcl.2014.11.031
44389168 71647 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 457 4 1 4 5.8 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCC1 10.1016/j.bmcl.2004.11.075
CHEMBL182154 71647 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 457 4 1 4 5.8 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCC1 10.1016/j.bmcl.2004.11.075
145991389 173783 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 6 1 6 6.5 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)NCc3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4288108 173783 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 6 1 6 6.5 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)NCc3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
145990051 173734 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 499 5 1 2 7.0 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C3CC3)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4287218 173734 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 499 5 1 2 7.0 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C3CC3)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
44410012 145177 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 9 3 7 4.1 CCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL377305 145177 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 9 3 7 4.1 CCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
71462272 88620 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 528 5 2 4 4.6 CN(C)C1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164502 88620 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 528 5 2 4 4.6 CN(C)C1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
71451563 88685 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 500 4 2 4 3.9 CN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164832 88685 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 500 4 2 4 3.9 CN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
145988286 173985 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 542 6 1 6 5.4 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-n5nccn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4291718 173985 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 542 6 1 6 5.4 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-n5nccn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
46880813 13148 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 442 3 1 4 4.4 Cc1noc(C)c1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1 10.1016/j.bmcl.2010.01.043
CHEMBL1082189 13148 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 442 3 1 4 4.4 Cc1noc(C)c1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1 10.1016/j.bmcl.2010.01.043
44409761 82641 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 9 3 7 4.4 CCc1nc(N)nc(NCC(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204880 82641 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 9 3 7 4.4 CCc1nc(N)nc(NCC(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11846625 84659 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 498 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(-c1ccccc1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
CHEMBL209394 84659 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 498 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(-c1ccccc1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
122178610 128125 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(N)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581043 128125 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(N)n2)cc1 10.1016/j.bmcl.2014.11.031
46880461 13007 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 439 4 1 3 4.4 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)CC3)cc2)c1 10.1016/j.bmcl.2010.01.043
CHEMBL1081483 13007 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 439 4 1 3 4.4 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)CC3)cc2)c1 10.1016/j.bmcl.2010.01.043
71453391 88621 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 5 2 4 4.2 CN(C)[C@@H]1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)C1 10.1016/j.bmc.2012.07.018
CHEMBL2164503 88621 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 5 2 4 4.2 CN(C)[C@@H]1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)C1 10.1016/j.bmc.2012.07.018
1221269 128812 12 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL359530 128812 12 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44389151 69279 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 445 6 1 4 5.7 CCN(CC)C(=O)c1ccccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
CHEMBL178138 69279 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 445 6 1 4 5.7 CCN(CC)C(=O)c1ccccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
71451564 88687 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)C(NC(=O)CN1CCN(C)CC1)(c1ccc(Cl)cc1)C(=O)N2 10.1016/j.bmc.2012.07.018
CHEMBL2164834 88687 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)C(NC(=O)CN1CCN(C)CC1)(c1ccc(Cl)cc1)C(=O)N2 10.1016/j.bmc.2012.07.018
71449753 88677 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 465 4 2 3 4.7 CC1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164825 88677 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 465 4 2 3 4.7 CC1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
44409871 82171 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 426 7 3 8 2.4 CN(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203948 82171 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 426 7 3 8 2.4 CN(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
46880569 12961 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1ccccc1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1 10.1016/j.bmcl.2010.01.043
CHEMBL1081212 12961 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1ccccc1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1 10.1016/j.bmcl.2010.01.043
70693640 79972 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 570 9 2 6 4.7 COc1ccccc1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
CHEMBL2011822 79972 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 570 9 2 6 4.7 COc1ccccc1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
CHEMBL449590 220741 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1074/jbc.m609796200
44576247 221001 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inverse agonist activity at human ghrelin receptor Val5:08Ala(Val216) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Val5:08Ala(Val216) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 221001 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inverse agonist activity at human ghrelin receptor Val5:08Ala(Val216) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Val5:08Ala(Val216) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
145994299 174175 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 523 5 1 4 6.1 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)NCc3cccc(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4295212 174175 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 523 5 1 4 6.1 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)NCc3cccc(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
71460577 88681 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 500 4 2 4 3.9 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)c(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164829 88681 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 500 4 2 4 3.9 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)c(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
16113902 144454 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL375859 144454 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
71462274 88624 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 528 5 2 4 3.8 CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1=O 10.1016/j.bmc.2012.07.018
CHEMBL2164506 88624 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 528 5 2 4 3.8 CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1=O 10.1016/j.bmc.2012.07.018
CHEMBL509976 222359 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human ghrelin receptor Ser3:08Ala(Ser123) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Ser3:08Ala(Ser123) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
70683143 79971 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 574 8 2 5 5.3 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(Cl)cc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011821 79971 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 574 8 2 5 5.3 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(Cl)cc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
46880495 13141 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)C[C@@H]3C)cc2)c1 10.1016/j.bmcl.2010.01.043
CHEMBL1082162 13141 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)C[C@@H]3C)cc2)c1 10.1016/j.bmcl.2010.01.043
11697618 69373 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 427 6 1 4 5.5 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Br)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178289 69373 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 427 6 1 4 5.5 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Br)noc2C)cc1 10.1016/j.bmcl.2004.11.075
145988557 174039 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 523 4 1 2 6.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C#CC3CC3)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4292914 174039 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 523 4 1 2 6.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C#CC3CC3)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
44409771 148031 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 461 6 3 7 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@@H]3CC4C=CC3C4)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL383073 148031 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 461 6 3 7 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@@H]3CC4C=CC3C4)cc2)cc1 10.1016/j.bmcl.2006.01.012
145980333 173360 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 577 6 1 4 7.5 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4280040 173360 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 577 6 1 4 7.5 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
11329138 71234 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at GHSR expressed in CHOK cells assessed as inhibition of ghrelin-induced increase in intracellular calcium levelAntagonist activity at GHSR expressed in CHOK cells assessed as inhibition of ghrelin-induced increase in intracellular calcium level
ChEMBL 481 9 1 5 5.1 CCN(CC)c1ccc(NC(=O)C2(N(C)C(=O)OCC(C)C)CCc3cccc(OC)c3C2)cc1 10.1021/jm0491750
CHEMBL181350 71234 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at GHSR expressed in CHOK cells assessed as inhibition of ghrelin-induced increase in intracellular calcium levelAntagonist activity at GHSR expressed in CHOK cells assessed as inhibition of ghrelin-induced increase in intracellular calcium level
ChEMBL 481 9 1 5 5.1 CCN(CC)c1ccc(NC(=O)C2(N(C)C(=O)OCC(C)C)CCc3cccc(OC)c3C2)cc1 10.1021/jm0491750
44576247 221001 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inverse agonist activity at human ghrelin receptor Met5:05Ala(Met213) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Met5:05Ala(Met213) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 221001 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inverse agonist activity at human ghrelin receptor Met5:05Ala(Met213) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Met5:05Ala(Met213) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
11568561 176333 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 447 7 1 5 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(OC)c1 10.1016/j.bmcl.2004.11.075
CHEMBL443560 176333 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 447 7 1 5 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(OC)c1 10.1016/j.bmcl.2004.11.075
145991945 173594 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 615 6 1 4 7.8 CCN(C(=O)N[C@@H](C)c1ccc(C#CC2CC2)c(Cl)c1Cl)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4284715 173594 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 615 6 1 4 7.8 CCN(C(=O)N[C@@H](C)c1ccc(C#CC2CC2)c(Cl)c1Cl)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1 10.1021/acs.jmedchem.8b00794
44394982 72912 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cellsAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells
ChEMBL 523 9 1 6 5.7 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL184093 72912 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cellsAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells
ChEMBL 523 9 1 6 5.7 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)CC1 10.1016/j.bmcl.2004.06.060
66788278 131970 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645254 131970 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
56942099 131972 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645256 131972 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
56942243 131974 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645258 131974 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 10.1016/j.bmcl.2016.04.003
127045858 146640 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 618 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2=CCCCO2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799225 146640 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 618 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2=CCCCO2)cc1 10.1016/j.bmcl.2016.04.003
70681018 79969 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 554 8 2 5 5.0 Cc1ccccc1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
CHEMBL2011819 79969 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 554 8 2 5 5.0 Cc1ccccc1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
70685225 80003 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 576 8 2 5 5.0 CC(C)[C@H](C(=O)N1CCC(NCc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011894 80003 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 576 8 2 5 5.0 CC(C)[C@H](C(=O)N1CCC(NCc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
11410373 145313 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 558 10 4 8 4.2 Cc1cc(C)cc(CNC(=O)CCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)c1 10.1016/j.bmcl.2006.01.012
CHEMBL377514 145313 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 558 10 4 8 4.2 Cc1cc(C)cc(CNC(=O)CCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)c1 10.1016/j.bmcl.2006.01.012
11339816 82782 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 446 8 3 7 4.7 Nc1nc(N)c(-c2ccc(NCc3ccnc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205521 82782 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 446 8 3 7 4.7 Nc1nc(N)c(-c2ccc(NCc3ccnc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
145992253 173707 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 595 6 1 6 6.4 COC(=O)c1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4286849 173707 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 595 6 1 6 6.4 COC(=O)c1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
11503585 71978 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 461 9 2 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCCO)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL182542 71978 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 461 9 2 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCCO)cc1 10.1016/j.bmcl.2004.06.060
44409762 82661 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 441 9 4 8 2.7 CCc1nc(N)nc(NCCO)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204884 82661 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 441 9 4 8 2.7 CCc1nc(N)nc(NCCO)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122180026 128365 0 None 8 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against ghrelin receptor (unknown origin) expressed in CHO cells assessed as inhibition of ghrelin-induced calcium responseAntagonist activity against ghrelin receptor (unknown origin) expressed in CHO cells assessed as inhibition of ghrelin-induced calcium response
ChEMBL 566 7 2 7 4.4 CC(=O)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586032 128365 0 None 8 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against ghrelin receptor (unknown origin) expressed in CHO cells assessed as inhibition of ghrelin-induced calcium responseAntagonist activity against ghrelin receptor (unknown origin) expressed in CHO cells assessed as inhibition of ghrelin-induced calcium response
ChEMBL 566 7 2 7 4.4 CC(=O)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
46880846 14384 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 442 3 1 3 4.4 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1088038 14384 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 442 3 1 3 4.4 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
44389248 128946 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 433 7 2 5 5.0 CCN(CCO)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL359714 128946 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 433 7 2 5 5.0 CCN(CCO)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
70695749 79985 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 562 9 2 6 4.3 CC(C)[C@H](C(=O)N1CCC(NCCC2CCOCC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011836 79985 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 562 9 2 6 4.3 CC(C)[C@H](C(=O)N1CCC(NCCC2CCOCC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
122178614 128129 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 660 13 2 7 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2C(=O)c2ccccc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581047 128129 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 660 13 2 7 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2C(=O)c2ccccc2)cc1 10.1016/j.bmcl.2014.11.031
70695748 79977 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 498 7 2 5 3.7 O=C1CN(CC(=O)NC2CCN(Cc3ccccc3)CC2)C(=O)c2cc(Oc3ccccc3)ccc2N1 10.1016/j.bmcl.2012.01.014
CHEMBL2011827 79977 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 498 7 2 5 3.7 O=C1CN(CC(=O)NC2CCN(Cc3ccccc3)CC2)C(=O)c2cc(Oc3ccccc3)ccc2N1 10.1016/j.bmcl.2012.01.014
145981687 173356 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 509 5 1 3 6.5 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(Cl)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4279987 173356 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 509 5 1 3 6.5 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(Cl)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
11508639 83310 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(Cl)cc2)cc1 10.1021/jm0510934
CHEMBL206091 83310 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(Cl)cc2)cc1 10.1021/jm0510934
44409683 83034 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 480 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205848 83034 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 480 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11626181 131159 2 None - 1 Human 6.5 pIC50 = 6.5 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 431 7 1 4 6.3 CCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL363896 131159 2 None - 1 Human 6.5 pIC50 = 6.5 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 431 7 1 4 6.3 CCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
11690097 83447 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 411 6 2 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(N(C)Cc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
CHEMBL206446 83447 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 411 6 2 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(N(C)Cc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
44409775 82800 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 8 3 7 3.7 CCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205605 82800 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 8 3 7 3.7 CCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44576247 221001 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inverse agonist activity at human wild type ghrelin receptor expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human wild type ghrelin receptor expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 221001 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inverse agonist activity at human wild type ghrelin receptor expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human wild type ghrelin receptor expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
11655355 81196 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)s3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL202642 81196 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)s3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
127047654 146755 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799883 146755 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
16113799 175492 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL436849 175492 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
145986080 173231 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 489 5 1 3 6.2 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(C)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4277793 173231 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 489 5 1 3 6.2 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(C)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
56942385 131976 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645260 131976 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
46880771 12682 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 448 3 1 4 4.4 C[C@H]1CN(C(=O)c2csc(-c3ccccc3F)n2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1079623 12682 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 448 3 1 4 4.4 C[C@H]1CN(C(=O)c2csc(-c3ccccc3F)n2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
11654867 82976 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 429 7 3 5 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(CCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205833 82976 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 429 7 3 5 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(CCc2ccccc2)n1 10.1021/jm0510934
122178600 128114 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581033 128114 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2)cc1 10.1016/j.bmcl.2014.11.031
46880844 14368 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 432 3 1 4 3.0 C[C@H]1CN(C(=O)c2ccc(N3CCOCC3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1087907 14368 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 432 3 1 4 3.0 C[C@H]1CN(C(=O)c2ccc(N3CCOCC3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
11248021 146033 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 454 8 4 6 4.3 Nc1nc(N)c(-c2ccc(NC(=O)NCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL378989 146033 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 454 8 4 6 4.3 Nc1nc(N)c(-c2ccc(NC(=O)NCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
122182189 128786 0 None -7 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assayAntagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assay
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593814 128786 0 None -7 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assayAntagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assay
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
44409865 147496 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 500 7 3 8 3.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN3Cc4ccccc4C3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL381759 147496 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 500 7 3 8 3.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN3Cc4ccccc4C3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11751384 148284 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 453 9 3 6 4.6 Nc1nc(N)c(-c2ccc(NC(=O)CCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL384524 148284 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 453 9 3 6 4.6 Nc1nc(N)c(-c2ccc(NC(=O)CCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
44409679 82283 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 466 8 4 8 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204322 82283 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 466 8 4 8 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409868 83517 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 487 9 3 7 4.9 CCc1nc(N)nc(NCc2ccccc2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206673 83517 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 487 9 3 7 4.9 CCc1nc(N)nc(NCc2ccccc2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409667 82744 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 451 6 3 7 4.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CCCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205294 82744 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 451 6 3 7 4.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CCCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44576247 221001 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 221001 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
56942388 146721 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799687 146721 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
11166495 82325 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 437 8 2 7 4.5 N#Cc1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL204474 82325 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 437 8 2 7 4.5 N#Cc1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
145994050 174124 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 615 6 1 6 7.1 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4294493 174124 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 615 6 1 6 7.1 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
11538533 81776 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203280 81776 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
46880770 12681 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 458 3 1 3 4.9 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3Cl)cn2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1079622 12681 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 458 3 1 3 4.9 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3Cl)cn2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
71453390 88618 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 526 6 2 4 4.4 C=CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164500 88618 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 526 6 2 4 4.4 C=CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
44409763 148143 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 487 6 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3Cc4ccccc4O3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL383757 148143 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 487 6 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3Cc4ccccc4O3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409989 172605 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 467 11 3 7 4.8 CCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL424860 172605 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 467 11 3 7 4.8 CCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44410008 148029 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 9 2 7 4.2 CCc1nc(N)nc(N(CC)CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL383058 148029 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 9 2 7 4.2 CCc1nc(N)nc(N(CC)CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11178309 86676 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 445 8 3 7 4.3 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL212415 86676 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 445 8 3 7 4.3 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
11517629 175117 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 431 6 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C)c1 10.1016/j.bmcl.2004.11.075
CHEMBL434330 175117 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 431 6 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C)c1 10.1016/j.bmcl.2004.11.075
127047655 146392 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797531 146392 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
127046957 146485 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 649 12 3 7 5.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc(F)cc(F)n2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798155 146485 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 649 12 3 7 5.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc(F)cc(F)n2)cc1 10.1016/j.bmcl.2016.04.003
127045858 146640 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 618 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2=CCCCO2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799225 146640 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 618 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2=CCCCO2)cc1 10.1016/j.bmcl.2016.04.003
56942098 131971 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645255 131971 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
127046957 146485 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 649 12 3 7 5.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc(F)cc(F)n2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798155 146485 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 649 12 3 7 5.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc(F)cc(F)n2)cc1 10.1016/j.bmcl.2016.04.003
46880630 12870 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 491 3 1 2 5.8 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3C(F)(F)F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080735 12870 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 491 3 1 2 5.8 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3C(F)(F)F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
70685219 79984 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 560 9 2 5 5.4 CC(C)[C@H](C(=O)N1CCC(NCCC2CCCCC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011835 79984 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 560 9 2 5 5.4 CC(C)[C@H](C(=O)N1CCC(NCCC2CCCCC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
16113245 128112 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581030 128112 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2014.11.031
122178607 128122 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 592 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncc(F)cc2F)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581040 128122 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 592 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncc(F)cc2F)cc1 10.1016/j.bmcl.2014.11.031
11452801 146076 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 417 7 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)C3CCCC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL379191 146076 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 417 7 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)C3CCCC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
46882763 12400 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-stimulated intracellular calcium mobilizationAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-stimulated intracellular calcium mobilization
ChEMBL 612 17 6 7 5.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1077617 12400 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-stimulated intracellular calcium mobilizationAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-stimulated intracellular calcium mobilization
ChEMBL 612 17 6 7 5.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
44409776 83918 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 7 3 7 3.5 CC(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL207754 83918 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 7 3 7 3.5 CC(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145991797 173695 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 613 5 1 6 6.5 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)NCc4ccc(-c5cnccn5)c(Cl)c4Cl)CC3)C2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4286597 173695 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 613 5 1 6 6.5 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)NCc4ccc(-c5cnccn5)c(Cl)c4Cl)CC3)C2)ncn1 10.1021/acs.jmedchem.8b00794
122178616 128130 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc3ccccc3cn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581048 128130 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc3ccccc3cn2)cc1 10.1016/j.bmcl.2014.11.031
11430583 86992 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 439 8 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL213704 86992 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 439 8 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL509976 222359 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human ghrelin receptor Phe3:04Ser(phe119) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Phe3:04Ser(phe119) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
11669486 71388 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 445 7 1 4 6.6 CCc1cc(N(CC)CC)ccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
CHEMBL181736 71388 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 445 7 1 4 6.6 CCc1cc(N(CC)CC)ccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
44409946 146593 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 514 7 3 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN3CCc4ccccc4C3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL379887 146593 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 514 7 3 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN3CCc4ccccc4C3)cc2)cc1 10.1016/j.bmcl.2006.01.012
127046806 146711 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 638 13 4 7 5.4 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799604 146711 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 638 13 4 7 5.4 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
122178600 128114 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581033 128114 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2)cc1 10.1016/j.bmcl.2014.11.031
11605333 83500 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 475 6 3 7 3.6 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Br)c1 10.1021/jm0510934
CHEMBL206589 83500 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 475 6 3 7 3.6 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Br)c1 10.1021/jm0510934
46880845 14383 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 460 3 1 3 4.5 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3F)c(F)c2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1088037 14383 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 460 3 1 3 4.5 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3F)c(F)c2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
46880773 12979 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3ccccn3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1081301 12979 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3ccccn3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
122178604 128118 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2N)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581037 128118 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2N)cc1 10.1016/j.bmcl.2014.11.031
56942387 146440 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 579 13 4 7 4.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797857 146440 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 579 13 4 7 4.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
44576247 221001 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inverse agonist activity at human ghrelin receptor Ile4:20Ala(Ile178) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ile4:20Ala(Ile178) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 221001 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inverse agonist activity at human ghrelin receptor Ile4:20Ala(Ile178) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ile4:20Ala(Ile178) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
11683469 83481 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 433 6 3 7 3.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(C)(=O)=O)c(F)c2)cc1 10.1021/jm0510934
CHEMBL206486 83481 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 433 6 3 7 3.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(C)(=O)=O)c(F)c2)cc1 10.1021/jm0510934
44389216 130632 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 442 6 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C#N)c1 10.1016/j.bmcl.2004.11.075
CHEMBL362595 130632 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 442 6 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C#N)c1 10.1016/j.bmcl.2004.11.075
145979819 173252 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 655 8 1 6 7.9 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4278185 173252 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 655 8 1 6 7.9 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
46880498 12767 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 507 4 1 3 5.7 C[C@H]1CN(C(=O)c2ccc(-c3cccc(OC(F)(F)F)c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080155 12767 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 507 4 1 3 5.7 C[C@H]1CN(C(=O)c2ccc(-c3cccc(OC(F)(F)F)c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
71462273 88623 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 513 5 2 3 5.7 CCN1CCCC(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)C1 10.1016/j.bmc.2012.07.018
CHEMBL2164505 88623 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 513 5 2 3 5.7 CCN1CCCC(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)C1 10.1016/j.bmc.2012.07.018
71453404 88678 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)N[C@]2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164826 88678 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)N[C@]2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
44389283 69719 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 403 5 1 4 5.7 CCN(C)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178494 69719 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 403 5 1 4 5.7 CCN(C)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
11179347 84128 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 490 9 2 8 4.0 CS(=O)(=O)c1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL208477 84128 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 490 9 2 8 4.0 CS(=O)(=O)c1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
44409764 83924 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 488 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL207792 83924 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 488 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11606121 71350 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 523 6 2 6 5.9 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.11.075
CHEMBL181584 71350 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 523 6 2 6 5.9 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.11.075
11539587 73851 1 None - 1 Human 6.3 pIC50 = 6.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 445 8 1 4 6.7 CCCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL187271 73851 1 None - 1 Human 6.3 pIC50 = 6.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 445 8 1 4 6.7 CCCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL3586019 218580 6 None - 1 Rat 8.3 pIC50 = 8.3 Functional
Inverse agonist activity at rat ghrelin receptor by inositol phosphate turnover assayInverse agonist activity at rat ghrelin receptor by inositol phosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CCCNC(=N)N)C(N)=O 10.1016/j.bmcl.2015.04.040
122178608 128123 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 570 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(C)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581041 128123 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 570 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(C)n2)cc1 10.1016/j.bmcl.2014.11.031
44409821 82812 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 564 10 4 8 4.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CCC(=O)NCc3cccc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205711 82812 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 564 10 4 8 4.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CCC(=O)NCc3cccc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11340044 148113 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(NCc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL383522 148113 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(NCc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
70683149 79998 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 504 8 2 5 3.9 CC(C)[C@H](C(=O)N1CCC(NCC2CC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011887 79998 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 504 8 2 5 3.9 CC(C)[C@H](C(=O)N1CCC(NCC2CC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
71452183 90304 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at ghrelin receptor assessed as inhibition of ghrelin-induced Ca2+ release by cell based assayAntagonist activity at ghrelin receptor assessed as inhibition of ghrelin-induced Ca2+ release by cell based assay
ChEMBL 538 5 4 6 1.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)N(C)C1=O 10.1021/jm1012374
CHEMBL2203623 90304 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at ghrelin receptor assessed as inhibition of ghrelin-induced Ca2+ release by cell based assayAntagonist activity at ghrelin receptor assessed as inhibition of ghrelin-induced Ca2+ release by cell based assay
ChEMBL 538 5 4 6 1.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)N(C)C1=O 10.1021/jm1012374
122178602 128116 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2Br)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581035 128116 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2Br)cc1 10.1016/j.bmcl.2014.11.031
11582836 69687 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 431 7 1 4 6.4 CCCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178463 69687 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 431 7 1 4 6.4 CCCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44389192 175425 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 471 4 1 4 6.2 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCCC1 10.1016/j.bmcl.2004.11.075
CHEMBL436275 175425 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 471 4 1 4 6.2 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCCC1 10.1016/j.bmcl.2004.11.075
71455106 88688 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 442 5 2 5 2.2 COc1ccc(C2(NC(=O)CN3CCN(C)CC3)C(=O)Nc3cc(Cl)c(C)cc32)cc1 10.1016/j.bmc.2012.07.018
CHEMBL2164835 88688 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 442 5 2 5 2.2 COc1ccc(C2(NC(=O)CN3CCN(C)CC3)C(=O)Nc3cc(Cl)c(C)cc32)cc1 10.1016/j.bmc.2012.07.018
44409998 145314 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 413 7 3 8 2.5 COCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL377515 145314 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 413 7 3 8 2.5 COCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145984632 173170 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 629 5 1 4 8.0 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)C(C)(C)C2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4276775 173170 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 629 5 1 4 8.0 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)C(C)(C)C2)ncn1 10.1021/acs.jmedchem.8b00794
10415364 133545 0 None -5 3 Human 7.3 pIC50 = 7.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL365294 133545 0 None -5 3 Human 7.3 pIC50 = 7.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
15949382 81623 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 6 3 8 3.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@@H]3CCCO3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203158 81623 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 6 3 8 3.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@@H]3CCCO3)cc2)cc1 10.1016/j.bmcl.2006.01.012
145993313 173671 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 577 7 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3cccc(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4286101 173671 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 577 7 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3cccc(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
11605822 131166 1 None - 1 Human 7.3 pIC50 = 7.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 503 9 1 6 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL363930 131166 1 None - 1 Human 7.3 pIC50 = 7.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 503 9 1 6 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCO2)cc1 10.1016/j.bmcl.2004.06.060
11154001 86663 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 406 7 4 6 3.6 CC(C)NC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
CHEMBL212354 86663 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 406 7 4 6 3.6 CC(C)NC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
44394930 73106 1 None - 1 Human 6.3 pIC50 = 6.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2cccc3c2OCO3)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL185028 73106 1 None - 1 Human 6.3 pIC50 = 6.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2cccc3c2OCO3)cc1 10.1016/j.bmcl.2004.06.060
11699004 72977 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 501 9 1 5 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL184429 72977 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 501 9 1 5 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)cc1 10.1016/j.bmcl.2004.06.060
11618705 173717 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 423 6 1 4 5.3 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL428698 173717 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 423 6 1 4 5.3 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)CC1 10.1016/j.bmcl.2004.06.060
44409785 82578 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 6 3 8 3.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@H]3CCCO3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204852 82578 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 6 3 8 3.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@H]3CCCO3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409990 83292 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 481 12 3 7 5.2 CCCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205995 83292 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 481 12 3 7 5.2 CCCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145992125 173529 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 552 5 2 5 6.2 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(N)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4283504 173529 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 552 5 2 5 6.2 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(N)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
46880568 13160 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 423 3 1 2 4.8 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1082211 13160 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 423 3 1 2 4.8 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
70687383 79999 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 525 9 2 4 6.6 CC(C)[C@H](C[C@H]1CC[C@@H](NCc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011890 79999 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 525 9 2 4 6.6 CC(C)[C@H](C[C@H]1CC[C@@H](NCc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
16113245 128112 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581030 128112 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL509976 222359 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Agonist activity at human ghrelin receptor Ser4:16Ala(Ser174) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Ser4:16Ala(Ser174) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
57422817 120226 18 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL 620 8 2 10 3.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/acs.jmedchem.1c02191
CHEMBL3319223 120226 18 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL 620 8 2 10 3.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/acs.jmedchem.1c02191
11190594 82760 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 469 10 3 8 3.9 CC(C)CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205445 82760 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 469 10 3 8 3.9 CC(C)CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
56942385 131976 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645260 131976 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
44576247 221001 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inverse agonist activity at human ghrelin receptor Phe3:04Ser(phe119) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Phe3:04Ser(phe119) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 221001 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inverse agonist activity at human ghrelin receptor Phe3:04Ser(phe119) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Phe3:04Ser(phe119) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
16113904 143814 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 550 12 3 6 5.1 COc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL374655 143814 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 550 12 3 6 5.1 COc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
44389215 69852 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccc(Cl)cc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178838 69852 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccc(Cl)cc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44576247 221001 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inverse agonist activity at human ghrelin receptor Asn7:02Ala(Asn305) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Asn7:02Ala(Asn305) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 221001 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inverse agonist activity at human ghrelin receptor Asn7:02Ala(Asn305) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Asn7:02Ala(Asn305) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
44409809 81840 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 10 3 7 4.4 CCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203578 81840 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 10 3 7 4.4 CCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
16113468 148578 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL386218 148578 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
11531313 69278 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 394 7 1 6 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3[N+](=O)[O-])noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178137 69278 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 394 7 1 6 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3[N+](=O)[O-])noc2C)cc1 10.1016/j.bmcl.2004.11.075
44389167 130636 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 425 7 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL362612 130636 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 425 7 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
46880674 12914 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccc(F)cc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080926 12914 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccc(F)cc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
71455085 88619 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 4 2 4 4.3 CN1CCCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164501 88619 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 4 2 4 4.3 CN1CCCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
46880463 13040 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)[C@H](C)C3)cc2)c1 10.1016/j.bmcl.2010.01.043
CHEMBL1081649 13040 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)[C@H](C)C3)cc2)c1 10.1016/j.bmcl.2010.01.043
46880812 12793 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 430 3 1 4 4.3 C[C@H]1CN(C(=O)c2ccc(-c3cncs3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080320 12793 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 430 3 1 4 4.3 C[C@H]1CN(C(=O)c2ccc(-c3cncs3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
46880497 13143 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 423 3 1 2 4.8 O=C(c1ccc(-c2ccccc2)cc1)N1CCCN(C(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/j.bmcl.2010.01.043
CHEMBL1082164 13143 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 423 3 1 2 4.8 O=C(c1ccc(-c2ccccc2)cc1)N1CCCN(C(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/j.bmcl.2010.01.043
44409770 148146 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 461 6 3 7 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@H]3CC4C=CC3C4)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL383766 148146 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 461 6 3 7 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@H]3CC4C=CC3C4)cc2)cc1 10.1016/j.bmcl.2006.01.012
122178604 128118 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2N)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581037 128118 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2N)cc1 10.1016/j.bmcl.2014.11.031
46880496 13142 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)C[C@H]3C)cc2)c1 10.1016/j.bmcl.2010.01.043
CHEMBL1082163 13142 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)C[C@H]3C)cc2)c1 10.1016/j.bmcl.2010.01.043
CHEMBL502208 220929 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1074/jbc.m609796200
145980382 173422 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4281310 173422 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
44389186 71389 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 379 7 1 5 4.8 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3OC)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL181739 71389 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 379 7 1 5 4.8 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3OC)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44409864 82274 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 502 9 3 8 4.0 CN(Cc1ccccc1)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204266 82274 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 502 9 3 8 4.0 CN(Cc1ccccc1)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409975 82565 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 411 7 3 7 3.3 CCc1nc(N)nc(NC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204835 82565 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 411 7 3 7 3.3 CCc1nc(N)nc(NC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409455 82743 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 487 6 3 7 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c2)cc1 10.1021/jm0510934
CHEMBL205286 82743 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 487 6 3 7 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c2)cc1 10.1021/jm0510934
11441554 7008 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 420 6 4 6 3.9 O=C(NC(C)(C)C)Nc1ccc(cc1)c1c(N)nc(nc1COCc1ccccc1)N 10.1021/jm060461g
5871 7008 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 420 6 4 6 3.9 O=C(NC(C)(C)C)Nc1ccc(cc1)c1c(N)nc(nc1COCc1ccccc1)N 10.1021/jm060461g
CHEMBL212761 7008 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 420 6 4 6 3.9 O=C(NC(C)(C)C)Nc1ccc(cc1)c1c(N)nc(nc1COCc1ccccc1)N 10.1021/jm060461g
11340329 86377 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 468 9 4 6 4.4 Nc1nc(N)c(-c2ccc(NC(=O)NCCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL211454 86377 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 468 9 4 6 4.4 Nc1nc(N)c(-c2ccc(NC(=O)NCCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
122178605 128119 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581038 128119 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2014.11.031
127047655 146392 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797531 146392 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
46880672 12968 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1ccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)[C@@H](C)C3)cc2)cc1 10.1016/j.bmcl.2010.01.043
CHEMBL1081254 12968 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1ccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)[C@@H](C)C3)cc2)cc1 10.1016/j.bmcl.2010.01.043
66601728 88616 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 5 2 4 4.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164499 88616 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 5 2 4 4.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
70689440 79968 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 554 8 2 5 5.0 Cc1ccc(Oc2ccc3c(c2)C(=O)N([C@@H](C(=O)NC2CCN(Cc4ccccc4)CC2)C(C)C)CC(=O)N3)cc1 10.1016/j.bmcl.2012.01.014
CHEMBL2011818 79968 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 554 8 2 5 5.0 Cc1ccc(Oc2ccc3c(c2)C(=O)N([C@@H](C(=O)NC2CCN(Cc4ccccc4)CC2)C(C)C)CC(=O)N3)cc1 10.1016/j.bmcl.2012.01.014
70693644 80002 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 496 9 1 3 6.7 CC(C)[C@H](C[C@H]1CC[C@@H](NCC2CC2)CC1)N1CCc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011893 80002 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 496 9 1 3 6.7 CC(C)[C@H](C[C@H]1CC[C@@H](NCC2CC2)CC1)N1CCc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
70695747 79966 0 None 1 2 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse GHSR1 receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at mouse GHSR1 receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011816 79966 0 None 1 2 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse GHSR1 receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at mouse GHSR1 receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
11225576 172816 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL425594 172816 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11225576 172816 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL425594 172816 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
122178608 128123 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 570 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(C)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581041 128123 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 570 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(C)n2)cc1 10.1016/j.bmcl.2014.11.031
122178609 128124 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 586 12 2 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(OC)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581042 128124 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 586 12 2 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(OC)n2)cc1 10.1016/j.bmcl.2014.11.031
56942388 146721 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799687 146721 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
56942535 146539 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 593 12 4 7 4.4 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798525 146539 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 593 12 4 7 4.4 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
11176805 84109 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 391 7 3 6 4.5 CC(C)(C)CNc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm0510934
CHEMBL208374 84109 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 391 7 3 6 4.5 CC(C)(C)CNc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm0510934
71453405 88686 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 462 5 2 5 2.6 COc1ccc(C2(NC(=O)CN3CCN(C)CC3)C(=O)Nc3cc(Cl)c(Cl)cc32)cc1 10.1016/j.bmc.2012.07.018
CHEMBL2164833 88686 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 462 5 2 5 2.6 COc1ccc(C2(NC(=O)CN3CCN(C)CC3)C(=O)Nc3cc(Cl)c(Cl)cc32)cc1 10.1016/j.bmc.2012.07.018
44394913 133951 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 537 10 1 5 7.5 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccccc2OC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL365721 133951 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 537 10 1 5 7.5 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccccc2OC)cc1 10.1016/j.bmcl.2004.06.060
44409832 83185 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 398 6 4 8 1.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205955 83185 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 398 6 4 8 1.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN)cc2)cc1 10.1016/j.bmcl.2006.01.012
25190383 88684 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164831 88684 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
122178615 128082 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2nccc3ccccc23)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3580668 128082 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2nccc3ccccc23)cc1 10.1016/j.bmcl.2014.11.031
44410013 83828 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 10 3 7 4.5 CCCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL207268 83828 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 10 3 7 4.5 CCCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44389243 71357 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 557 7 1 6 6.2 O=C(Nc1ccccc1C(=O)N1CCCCC1)c1c(-c2c(Cl)cccc2Cl)noc1CCC1OCCCO1 10.1016/j.bmcl.2004.11.075
CHEMBL181619 71357 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 557 7 1 6 6.2 O=C(Nc1ccccc1C(=O)N1CCCCC1)c1c(-c2c(Cl)cccc2Cl)noc1CCC1OCCCO1 10.1016/j.bmcl.2004.11.075
753168 130017 40 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 349 6 1 4 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL361366 130017 40 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 349 6 1 4 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
46880566 13158 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 491 3 1 2 5.8 C[C@H]1CN(C(=O)c2ccc(-c3cccc(C(F)(F)F)c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1082209 13158 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 491 3 1 2 5.8 C[C@H]1CN(C(=O)c2ccc(-c3cccc(C(F)(F)F)c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
122178603 128117 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 590 11 2 6 6.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(Cl)nc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581036 128117 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 590 11 2 6 6.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(Cl)nc2)cc1 10.1016/j.bmcl.2014.11.031
44409979 147337 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 7 2 7 3.4 CCc1nc(N)nc(N(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL381159 147337 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 7 2 7 3.4 CCc1nc(N)nc(N(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11256439 82154 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 344 5 3 6 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C#N)cc2)cc1 10.1021/jm0510934
CHEMBL203843 82154 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 344 5 3 6 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C#N)cc2)cc1 10.1021/jm0510934
11655578 176812 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 462 8 3 7 5.2 Nc1nc(N)c(-c2ccc(NCc3cnc4ccccc4c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL444277 176812 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 462 8 3 7 5.2 Nc1nc(N)c(-c2ccc(NCc3cnc4ccccc4c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
70681019 79974 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 570 9 2 6 4.7 COc1ccc(Oc2ccc3c(c2)C(=O)N([C@@H](C(=O)NC2CCN(Cc4ccccc4)CC2)C(C)C)CC(=O)N3)cc1 10.1016/j.bmcl.2012.01.014
CHEMBL2011824 79974 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 570 9 2 6 4.7 COc1ccc(Oc2ccc3c(c2)C(=O)N([C@@H](C(=O)NC2CCN(Cc4ccccc4)CC2)C(C)C)CC(=O)N3)cc1 10.1016/j.bmcl.2012.01.014
122178612 128127 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 572 11 2 6 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc[n+]2[O-])cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581045 128127 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 572 11 2 6 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc[n+]2[O-])cc1 10.1016/j.bmcl.2014.11.031
11617435 82772 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 359 5 3 6 4.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2csc(Cl)c2)cc1 10.1021/jm0510934
CHEMBL205486 82772 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 359 5 3 6 4.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2csc(Cl)c2)cc1 10.1021/jm0510934
145988647 173851 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4ncccn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4289530 173851 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4ncccn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
11663710 131245 1 None - 1 Human 8.1 pIC50 = 8.1 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 528 9 1 5 6.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL363995 131245 1 None - 1 Human 8.1 pIC50 = 8.1 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 528 9 1 5 6.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
56942099 131972 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645256 131972 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
56942242 131973 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645257 131973 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 10.1016/j.bmcl.2016.04.003
11663710 131245 1 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilizationAntagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilization
ChEMBL 528 9 1 5 6.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)cc1 10.1016/j.bmcl.2012.01.014
CHEMBL363995 131245 1 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilizationAntagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilization
ChEMBL 528 9 1 5 6.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)cc1 10.1016/j.bmcl.2012.01.014
70695747 79966 0 None -1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011816 79966 0 None -1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
70687380 79980 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)N1CCC(NCc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011831 79980 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)N1CCC(NCc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
122178605 128119 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581038 128119 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2014.11.031
145988894 173923 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4290680 173923 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
16203569 148511 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL385803 148511 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
145981343 173488 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 669 6 1 6 7.6 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@H](c3ccc(-c4cnccn4)c(Cl)c3Cl)C(F)(F)F)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4282719 173488 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 669 6 1 6 7.6 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@H](c3ccc(-c4cnccn4)c(Cl)c3Cl)C(F)(F)F)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL509976 222359 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human ghrelin receptor Phe7:06Leu(Phe306) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Phe7:06Leu(Phe306) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
122178615 128082 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2nccc3ccccc23)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3580668 128082 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2nccc3ccccc23)cc1 10.1016/j.bmcl.2014.11.031
44409810 147678 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 469 9 3 9 2.8 CCOC(=O)CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL382138 147678 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 469 9 3 9 2.8 CCOC(=O)CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
16113124 128113 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccncc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581032 128113 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccncc2)cc1 10.1016/j.bmcl.2014.11.031
44576247 221001 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inverse agonist activity at human ghrelin receptor Ser5:09Ala(Ser217) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ser5:09Ala(Ser217) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 221001 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inverse agonist activity at human ghrelin receptor Ser5:09Ala(Ser217) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ser5:09Ala(Ser217) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
44409536 82284 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 579 9 3 8 5.2 Nc1nc(N)c(-c2ccc(NCc3cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL204325 82284 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 579 9 3 8 5.2 Nc1nc(N)c(-c2ccc(NCc3cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
145992835 173613 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cncnc4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4285075 173613 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cncnc4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
11327400 82147 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 412 8 3 7 4.0 Nc1nc(N)c(-c2ccc(NCc3ccncc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL203782 82147 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 412 8 3 7 4.0 Nc1nc(N)c(-c2ccc(NCc3ccncc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
11539588 73687 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 445 7 1 4 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C(C)C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL186540 73687 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 445 7 1 4 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C(C)C)cc1 10.1016/j.bmcl.2004.06.060
16113796 91456 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL222518 91456 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
11442040 85326 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 440 7 4 6 4.7 Nc1nc(N)c(-c2ccc(NC(=O)Nc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL211211 85326 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 440 7 4 6 4.7 Nc1nc(N)c(-c2ccc(NC(=O)Nc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
122178601 128115 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cncc(Br)c2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581034 128115 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cncc(Br)c2)cc1 10.1016/j.bmcl.2014.11.031
56942243 131974 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645258 131974 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 10.1016/j.bmcl.2016.04.003
46880725 13031 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 455 3 1 2 5.3 Cc1ccccc1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1F 10.1016/j.bmcl.2010.01.043
CHEMBL1081612 13031 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 455 3 1 2 5.3 Cc1ccccc1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1F 10.1016/j.bmcl.2010.01.043
122178609 128124 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 586 12 2 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(OC)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581042 128124 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 586 12 2 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(OC)n2)cc1 10.1016/j.bmcl.2014.11.031
11454617 148097 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 488 8 3 8 4.0 CN(Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2006.01.012
CHEMBL383411 148097 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 488 8 3 8 4.0 CN(Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2006.01.012
46880628 12804 0 None -4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080389 12804 0 None -4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
44409684 147663 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 474 8 4 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL382033 147663 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 474 8 4 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409672 147265 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 479 9 3 9 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccco3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL380971 147265 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 479 9 3 9 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccco3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409673 83525 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 493 9 3 9 3.9 Cc1ccc(COCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)o1 10.1016/j.bmcl.2006.01.012
CHEMBL206741 83525 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 493 9 3 9 3.9 Cc1ccc(COCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)o1 10.1016/j.bmcl.2006.01.012
11453509 82953 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 441 9 3 7 4.6 COc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL205784 82953 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 441 9 3 7 4.6 COc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
127047362 146497 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 590 11 5 7 4.7 COc1ccc(Cn2c([C@H](N)Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798204 146497 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 590 11 5 7 4.7 COc1ccc(Cn2c([C@H](N)Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
56942535 146539 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 593 12 4 7 4.4 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798525 146539 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 593 12 4 7 4.4 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
145990956 173800 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 509 4 1 2 6.6 C[C@H](NC(=O)N(C)C1CCN(C2CCc3ccccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4288441 173800 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 509 4 1 2 6.6 C[C@H](NC(=O)N(C)C1CCN(C2CCc3ccccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
44394947 176002 1 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL440939 176002 1 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)cc1 10.1016/j.bmcl.2004.06.060
44410007 83202 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 438 8 4 8 2.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205963 83202 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 438 8 4 8 2.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11583811 82762 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 479 8 3 6 5.7 Nc1nc(N)c(-c2ccc(NCc3ccc(C(F)(F)F)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205450 82762 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 479 8 3 6 5.7 Nc1nc(N)c(-c2ccc(NCc3ccc(C(F)(F)F)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
11576960 73889 1 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 500 8 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL187427 73889 1 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 500 8 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
11281346 82793 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 411 8 3 6 4.6 Nc1nc(N)c(-c2ccc(NCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205568 82793 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 411 8 3 6 4.6 Nc1nc(N)c(-c2ccc(NCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL499371 220874 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCC(N)=O)C(N)=O 10.1074/jbc.m609796200
155540883 179736 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assayCompetitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4517399 179736 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assayCompetitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
155540883 179736 0 None - 1 Human 8.0 pKd = 8.0 Functional
Competitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assayCompetitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4517399 179736 0 None - 1 Human 8.0 pKd = 8.0 Functional
Competitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assayCompetitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
155557019 181366 0 None - 1 Human 7.5 pKd = 7.5 Functional
Competitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assayCompetitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4556887 181366 0 None - 1 Human 7.5 pKd = 7.5 Functional
Competitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assayCompetitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
155557019 181366 0 None - 1 Human 7.1 pKd = 7.1 Functional
Competitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assayCompetitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4556887 181366 0 None - 1 Human 7.1 pKd = 7.1 Functional
Competitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assayCompetitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
57399248 75819 0 None - 1 Human 9.0 pKi = 9 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm1012374
CHEMBL1923617 75819 0 None - 1 Human 9.0 pKi = 9 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm1012374
71452183 90304 0 None - 1 Human 7.0 pKi = 7 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 538 5 4 6 1.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)N(C)C1=O 10.1021/jm1012374
CHEMBL2203623 90304 0 None - 1 Human 7.0 pKi = 7 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 538 5 4 6 1.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)N(C)C1=O 10.1021/jm1012374
44454117 162335 0 None - 1 Human 7.9 pKi = 7.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
CHEMBL404336 162335 0 None - 1 Human 7.9 pKi = 7.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
44454060 162111 0 None - 1 Human 5.9 pKi = 5.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL403180 162111 0 None - 1 Human 5.9 pKi = 5.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
44454367 102036 0 None - 1 Human 7.8 pKi = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
CHEMBL256235 102036 0 None - 1 Human 7.8 pKi = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
44454338 104611 0 None - 1 Human 6.7 pKi = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL272085 104611 0 None - 1 Human 6.7 pKi = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
44434080 96686 0 None - 1 Human 6.7 pKi = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL237933 96686 0 None - 1 Human 6.7 pKi = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2008.01.100
44454302 166159 0 None - 1 Human 6.6 pKi = 6.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
CHEMBL410060 166159 0 None - 1 Human 6.6 pKi = 6.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
44454092 104425 0 None - 1 Human 5.6 pKi = 5.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
CHEMBL271082 104425 0 None - 1 Human 5.6 pKi = 5.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
44454432 162037 0 None - 1 Human 5.6 pKi = 5.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
CHEMBL402808 162037 0 None - 1 Human 5.6 pKi = 5.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
9950632 95481 0 None - 1 Human 5.5 pKi = 5.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.01.100
CHEMBL236038 95481 0 None - 1 Human 5.5 pKi = 5.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.01.100
44454399 161918 0 None - 1 Human 6.5 pKi = 6.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 447 11 2 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC(C#N)Cc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL402086 161918 0 None - 1 Human 6.5 pKi = 6.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 447 11 2 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC(C#N)Cc1ccccc1 10.1016/j.bmcl.2008.01.100
44454432 162037 0 None - 1 Human 5.4 pKi = 5.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
CHEMBL402808 162037 0 None - 1 Human 5.4 pKi = 5.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
25022640 104577 0 None - 1 Human 7.4 pKi = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
CHEMBL271876 104577 0 None - 1 Human 7.4 pKi = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
44454092 104425 0 None - 1 Human 6.3 pKi = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
CHEMBL271082 104425 0 None - 1 Human 6.3 pKi = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
44454303 104345 0 None - 1 Human 8.2 pKi = 8.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
CHEMBL270666 104345 0 None - 1 Human 8.2 pKi = 8.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
44454304 104379 0 None - 1 Human 6.3 pKi = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
CHEMBL270876 104379 0 None - 1 Human 6.3 pKi = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
56926461 75811 0 None - 1 Human 8.2 pKi = 8.2 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm1012374
CHEMBL1923609 75811 0 None - 1 Human 8.2 pKi = 8.2 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm1012374
44454398 104374 0 None - 1 Human 6.2 pKi = 6.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 447 11 2 8 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(C#N)c1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL270851 104374 0 None - 1 Human 6.2 pKi = 6.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 447 11 2 8 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(C#N)c1ccccc1 10.1016/j.bmcl.2008.01.100
44454060 162111 0 None - 1 Human 7.2 pKi = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL403180 162111 0 None - 1 Human 7.2 pKi = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
44454367 102036 0 None - 1 Human 6.2 pKi = 6.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
CHEMBL256235 102036 0 None - 1 Human 6.2 pKi = 6.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
44454337 162382 0 None - 1 Human 8.1 pKi = 8.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL404545 162382 0 None - 1 Human 8.1 pKi = 8.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
44454117 162335 0 None - 1 Human 6.1 pKi = 6.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
CHEMBL404336 162335 0 None - 1 Human 6.1 pKi = 6.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
1099 8568 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Measuring ghrelin-induced GHSR activation detected by β-arrestin recruitment in cells stably expressing hGHSR.Measuring ghrelin-induced GHSR activation detected by β-arrestin recruitment in cells stably expressing hGHSR.
Guide to Pharmacology None None None None 29233536
121879 9015 24 None -3 5 Human 7.0 pEC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 15905359
5868 9015 24 None -3 5 Human 7.0 pEC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 15905359
CHEMBL308716 9015 24 None -3 5 Human 7.0 pEC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 15905359
5869 10852 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21402696
121879 9015 24 None 1 5 Rat 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 8503009
5868 9015 24 None 1 5 Rat 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 8503009
CHEMBL308716 9015 24 None 1 5 Rat 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 8503009
1099 8568 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10628755
1099 8568 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
121879 9015 24 None -3 5 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 15905359
5868 9015 24 None -3 5 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 15905359
CHEMBL308716 9015 24 None -3 5 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 15905359
1093 8575 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
4345065 8575 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
1093 8575 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
4345065 8575 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
178024 8752 33 None -1 3 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10427162
178024 8752 33 None -1 3 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 15905359
5867 8752 33 None -1 3 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10427162
5867 8752 33 None -1 3 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 15905359
CHEMBL13817 8752 33 None -1 3 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10427162
CHEMBL13817 8752 33 None -1 3 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 15905359
1099 8568 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12907757
1099 8568 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21402696
5866 10396 4 None - 1 Human 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 18923064
9804743 10396 4 None - 1 Human 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 18923064
CHEMBL360227 10396 4 None - 1 Human 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 18923064
9734 9110 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
IC<sub>50</sub> for LEAP2 antagonism of GHSR activation in the presence of ghrelin.IC<sub>50</sub> for LEAP2 antagonism of GHSR activation in the presence of ghrelin.
Guide to Pharmacology None None None None 29233536
11441554 7008 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 6 4 6 3.9 O=C(NC(C)(C)C)Nc1ccc(cc1)c1c(N)nc(nc1COCc1ccccc1)N 16854051
5871 7008 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 6 4 6 3.9 O=C(NC(C)(C)C)Nc1ccc(cc1)c1c(N)nc(nc1COCc1ccccc1)N 16854051
CHEMBL212761 7008 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 6 4 6 3.9 O=C(NC(C)(C)C)Nc1ccc(cc1)c1c(N)nc(nc1COCc1ccccc1)N 16854051
5872 8905 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 603 10 3 8 5.4 COc1ccc(c(c1)OC)n1c(nnc1n1cc(c2c1cccc2)CC)[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H]1CCCN1 17927165
74015851 8905 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 603 10 3 8 5.4 COc1ccc(c(c1)OC)n1c(nnc1n1cc(c2c1cccc2)CC)[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H]1CCCN1 17927165
25124566 8655 8 None 2 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 20593439
5870 8655 8 None 2 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 20593439
CHEMBL3358452 8655 8 None 2 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 20593439
5866 10396 4 None - 1 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 11741481
9804743 10396 4 None - 1 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 11741481
CHEMBL360227 10396 4 None - 1 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 11741481
25124566 8655 8 None -2 2 Rat 8.0 pKB = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 21034740
5870 8655 8 None -2 2 Rat 8.0 pKB = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 21034740
CHEMBL3358452 8655 8 None -2 2 Rat 8.0 pKB = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 21034740


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Ligands Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Affinity)		 # tested GPCRs
(Affinity)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
2713 212050 82 None - 0 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5353524 212050 82 None - 0 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5360566 212050 82 None - 0 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
88536661 212050 82 None - 0 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
9552079 212050 82 None - 0 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1330113 212050 82 None - 0 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL790 212050 82 None - 0 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
156419 7725 74 None - 1 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
3308 7725 74 None - 1 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
647 7725 74 None - 1 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL1201284 7725 74 None - 1 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
DB01012 7725 74 None - 1 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
5920 54049 83 None - 1 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 651 5 3 4 4.0 N[C@@H](Cc1cc(I)c(Oc2ccc(O)c(I)c2)c(I)c1)C(=O)O 10.1038/s41467-023-40064-9
7048703 54049 83 None - 1 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 651 5 3 4 4.0 N[C@@H](Cc1cc(I)c(Oc2ccc(O)c(I)c2)c(I)c1)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL1544 54049 83 None - 1 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 651 5 3 4 4.0 N[C@@H](Cc1cc(I)c(Oc2ccc(O)c(I)c2)c(I)c1)C(=O)O 10.1038/s41467-023-40064-9
148192 17192 81 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 704 14 5 9 4.2 COC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)[C@@H](O)CN(Cc1ccc(-c2ccccn2)cc1)NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)C(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL1163 17192 81 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 704 14 5 9 4.2 COC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)[C@@H](O)CN(Cc1ccc(-c2ccccn2)cc1)NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)C(C)(C)C 10.1038/s41467-023-40064-9
154257 185398 67 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
CHEMBL46740 185398 67 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
2600 10551 74 None - 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 10551 74 None - 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 10551 74 None - 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 10551 74 None - 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 10551 74 None - 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
47319 33237 35 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 929 24 0 12 8.1 COc1ccc(CC2c3cc(OC)c(OC)cc3CC[N+]2(C)CCC(=O)OCCCCCOC(=O)CC[N+]2(C)CCc3cc(OC)c(OC)cc3C2Cc2ccc(OC)c(OC)c2)cc1OC 10.1038/s41467-023-40064-9
CHEMBL1360 33237 35 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 929 24 0 12 8.1 COc1ccc(CC2c3cc(OC)c(OC)cc3CC[N+]2(C)CCC(=O)OCCCCCOC(=O)CC[N+]2(C)CCc3cc(OC)c(OC)cc3C2Cc2ccc(OC)c(OC)c2)cc1OC 10.1038/s41467-023-40064-9
135409453 10545 41 None - 2 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 10545 41 None - 2 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 10545 41 None - 2 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
71496458 122342 87 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
CHEMBL3353410 122342 87 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
242 7258 124 None - 51 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 7258 124 None - 51 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 7258 124 None - 51 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 7258 124 None - 51 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 7258 124 None - 51 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
39186 92710 54 None - 2 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 414 6 0 6 3.4 COc1ccc([C@@H]2Sc3ccccc3N(CCN(C)C)C(=O)[C@@H]2OC(C)=O)cc1 10.1038/s41467-023-40064-9
CHEMBL23 92710 54 None - 2 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 414 6 0 6 3.4 COc1ccc([C@@H]2Sc3ccccc3N(CCN(C)C)C(=O)[C@@H]2OC(C)=O)cc1 10.1038/s41467-023-40064-9
16362 9899 71 None - 29 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2172 9899 71 None - 29 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
90 9899 71 None - 29 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1423 9899 71 None - 29 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01100 9899 71 None - 29 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
3042 8196 35 None - 15 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
355 8196 35 None - 15 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
868 8196 35 None - 15 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
CHEMBL1123 8196 35 None - 15 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
DB00804 8196 35 None - 15 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
10184665 10763 51 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
4799 10763 51 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
7353 10763 51 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
CHEMBL1198857 10763 51 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
DB09082 10763 51 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
3191 109635 97 None - 25 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
CHEMBL305660 109635 97 None - 25 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
DB11742 109635 97 None - 25 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
3926 214020 40 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 491 9 1 3 5.8 Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL92870 214020 40 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 491 9 1 3 5.8 Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
11626560 207716 94 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
CHEMBL601719 207716 94 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
2267 7347 71 None - 7 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
271 7347 71 None - 7 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
7121 7347 71 None - 7 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL639 7347 71 None - 7 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
DB00972 7347 71 None - 7 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
135564886 21265 5 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
135673376 21265 5 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
137157436 21265 5 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
145948239 21265 5 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
71587099 21265 5 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
CHEMBL1201304 21265 5 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
2585 7590 103 None - 22 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
522 7590 103 None - 22 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
551 7590 103 None - 22 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
CHEMBL723 7590 103 None - 22 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
DB01136 7590 103 None - 22 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
1353 8692 93 None - 85 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 8692 93 None - 85 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 8692 93 None - 85 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 8692 93 None - 85 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 8692 93 None - 85 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
100 10577 58 None - 54 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
2637 10577 58 None - 54 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
5452 10577 58 None - 54 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
CHEMBL479 10577 58 None - 54 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
DB00679 10577 58 None - 54 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
202 8290 77 None - 33 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
60835 8290 77 None - 33 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
972 8290 77 None - 33 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1175 8290 77 None - 33 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
DB00476 8290 77 None - 33 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
11976 7707 59 None - 24 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
667467 7707 59 None - 24 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
CHEMBL908 7707 59 None - 24 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
DB01239 7707 59 None - 24 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
2218 22055 23 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 322 8 0 2 4.4 CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1 10.1038/s41467-023-40064-9
CHEMBL1213033 22055 23 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 322 8 0 2 4.4 CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1 10.1038/s41467-023-40064-9
41684 37995 105 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
CHEMBL1401 37995 105 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
3025 14047 86 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 10 1 4 3.5 CCCCOc1cc(C(=O)NCCN(CC)CC)c2ccccc2n1 10.1038/s41467-023-40064-9
CHEMBL1086 14047 86 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 10 1 4 3.5 CCCCOc1cc(C(=O)NCCN(CC)CC)c2ccccc2n1 10.1038/s41467-023-40064-9
44112 128068 48 None - 7 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 10.1038/s41467-023-40064-9
CHEMBL357995 128068 48 None - 7 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 10.1038/s41467-023-40064-9
68617 212306 62 None - 26 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1709 212306 62 None - 26 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL809 212306 62 None - 26 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
2726 7706 68 None - 72 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 7706 68 None - 72 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 7706 68 None - 72 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 7706 68 None - 72 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 7706 68 None - 72 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
16363 7383 53 None - 7 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
312 7383 53 None - 7 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
9215 7383 53 None - 7 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL297302 7383 53 None - 7 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB12867 7383 53 None - 7 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2291 9958 58 None - 12 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
2561 9958 58 None - 12 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
4932 9958 58 None - 12 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL631 9958 58 None - 12 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
DB01182 9958 58 None - 12 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
24826799 17570 104 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 532 4 1 6 4.5 Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12 10.1038/s41467-023-40064-9
CHEMBL1171837 17570 104 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 532 4 1 6 4.5 Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12 10.1038/s41467-023-40064-9
2274 9947 58 None - 31 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4917 9947 58 None - 31 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
7279 9947 58 None - 31 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL728 9947 58 None - 31 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00433 9947 58 None - 31 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
2398 7741 62 None - 29 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801 7741 62 None - 29 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
701 7741 62 None - 29 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL415 7741 62 None - 29 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB01242 7741 62 None - 29 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
4046 9261 33 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4252 9261 33 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
CHEMBL416956 9261 33 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
DB00358 9261 33 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
3074 24730 26 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 604 16 0 12 3.5 COc1cc(C(=O)OCCCN2CCCN(CCCOC(=O)c3cc(OC)c(OC)c(OC)c3)CC2)cc(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL126075 24730 26 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 604 16 0 12 3.5 COc1cc(C(=O)OCCCN2CCCN(CCCOC(=O)c3cc(OC)c(OC)c(OC)c3)CC2)cc(OC)c1OC 10.1038/s41467-023-40064-9
4413 104849 57 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 347 4 5 4 2.6 N=C(N)Nc1ccc(C(=O)Oc2ccc3cc(C(=N)N)ccc3c2)cc1 10.1038/s41467-023-40064-9
CHEMBL273264 104849 57 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 347 4 5 4 2.6 N=C(N)Nc1ccc(C(=O)Oc2ccc3cc(C(=N)N)ccc3c2)cc1 10.1038/s41467-023-40064-9
25382 15929 37 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL110094 15929 37 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
2375 165173 106 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 430 5 2 5 2.9 CC(O)(CS(=O)(=O)c1ccc(F)cc1)C(=O)Nc1ccc(C#N)c(C(F)(F)F)c1 10.1038/s41467-023-40064-9
CHEMBL409 165173 106 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 430 5 2 5 2.9 CC(O)(CS(=O)(=O)c1ccc(F)cc1)C(=O)Nc1ccc(C#N)c(C(F)(F)F)c1 10.1038/s41467-023-40064-9
2351 11072 49 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1008 11072 49 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1257078 11072 49 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
448537 167029 89 None - 25 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL411 167029 89 None - 25 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 10.1038/s41467-023-40064-9
3393 214703 24 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 387 6 0 3 4.0 CCN(CC)CCN1C(=O)CN=C(c2ccccc2F)c2cc(Cl)ccc21 10.1038/s41467-023-40064-9
CHEMBL968 214703 24 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 387 6 0 3 4.0 CCN(CC)CCN1C(=O)CN=C(c2ccccc2F)c2cc(Cl)ccc21 10.1038/s41467-023-40064-9
441243 16608 58 None - 8 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 670 12 5 7 3.1 CC(C)(C)NC(=O)[C@@H]1C[C@@H]2CCCC[C@@H]2CN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)c1ccc2ccccc2n1 10.1038/s41467-023-40064-9
CHEMBL114 16608 58 None - 8 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 670 12 5 7 3.1 CC(C)(C)NC(=O)[C@@H]1C[C@@H]2CCCC[C@@H]2CN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)c1ccc2ccccc2n1 10.1038/s41467-023-40064-9
214 10632 58 None - 30 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 10632 58 None - 30 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 10632 58 None - 30 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 10632 58 None - 30 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 10632 58 None - 30 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 10632 58 None - 30 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
3036780 114308 20 None - 53 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
46780481 114308 20 None - 53 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
9903970 114308 20 None - 53 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3187365 114308 20 None - 53 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3544974 114308 20 None - 53 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL504548 114308 20 None - 53 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
DB06216 114308 20 None - 53 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
6436173 61890 45 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL1617 61890 45 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
8550 21196 57 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 578 7 1 9 4.2 COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5ccccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC 10.1038/s41467-023-40064-9
CHEMBL1200515 21196 57 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 578 7 1 9 4.2 COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5ccccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC 10.1038/s41467-023-40064-9
31101 7516 40 None - 35 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
35 7516 40 None - 35 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
403 7516 40 None - 35 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
CHEMBL493 7516 40 None - 35 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
DB01200 7516 40 None - 35 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
104850 10103 96 None - 6 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
4150 10103 96 None - 6 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
743 10103 96 None - 6 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL111 10103 96 None - 6 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
DB06155 10103 96 None - 6 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
392622 63086 95 None - 4 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
CHEMBL163 63086 95 None - 4 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
2995 211184 53 None - 23 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1696 211184 53 None - 23 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL72 211184 53 None - 23 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
DB01151 211184 53 None - 23 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
3947 213174 53 None - 16 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL87708 213174 53 None - 16 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
212 10578 47 None - 25 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2639 10578 47 None - 25 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651 10578 47 None - 25 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL1201 10578 47 None - 25 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01623 10578 47 None - 25 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
73348210 217728 0 None - 0 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](c2ccccc2)NC(=O)[C@@H]2C[C@H](OC(=O)NCCN)CN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(OCc3ccccc3)cc2)NC1=O 10.1038/s41467-023-40064-9
CHEMBL3039583 217728 0 None - 0 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](c2ccccc2)NC(=O)[C@@H]2C[C@H](OC(=O)NCCN)CN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(OCc3ccccc3)cc2)NC1=O 10.1038/s41467-023-40064-9
nan 217728 0 None - 0 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](c2ccccc2)NC(=O)[C@@H]2C[C@H](OC(=O)NCCN)CN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(OCc3ccccc3)cc2)NC1=O 10.1038/s41467-023-40064-9
60065 91144 6 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 505 7 1 8 4.2 COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@@H]2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL2218858 91144 6 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 505 7 1 8 4.2 COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@@H]2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
3081361 100709 123 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
CHEMBL24828 100709 123 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
107771 127026 49 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 517 7 2 7 6.1 COc1ccc2nc3cc(Cl)ccc3c(Nc3cc(CN4CCCC4)c(O)c(CN4CCCC4)c3)c2n1 10.1038/s41467-023-40064-9
CHEMBL35228 127026 49 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 517 7 2 7 6.1 COc1ccc2nc3cc(Cl)ccc3c(Nc3cc(CN4CCCC4)c(O)c(CN4CCCC4)c3)c2n1 10.1038/s41467-023-40064-9
3151 8244 97 None - 26 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
945 8244 97 None - 26 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
965 8244 97 None - 26 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL219916 8244 97 None - 26 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01184 8244 97 None - 26 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
3949 107390 50 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 468 8 0 5 4.9 COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL29188 107390 50 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 468 8 0 5 4.9 COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC 10.1038/s41467-023-40064-9
2435 10362 83 None - 48 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
60149 10362 83 None - 48 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
98 10362 83 None - 48 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
CHEMBL12713 10362 83 None - 48 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
DB06144 10362 83 None - 48 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
25181577 84994 56 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 574 9 2 9 5.0 CCOC(=O)[C@@H](N)Cc1ccc(-c2cc(O[C@H](c3ccc(Cl)cc3-n3ccc(C)n3)C(F)(F)F)nc(N)n2)cc1 10.1038/s41467-023-40064-9
CHEMBL2105695 84994 56 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 574 9 2 9 5.0 CCOC(=O)[C@@H](N)Cc1ccc(-c2cc(O[C@H](c3ccc(Cl)cc3-n3ccc(C)n3)C(F)(F)F)nc(N)n2)cc1 10.1038/s41467-023-40064-9
2318 161635 29 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 351 7 1 3 4.1 CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL400599 161635 29 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 351 7 1 3 4.1 CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1 10.1038/s41467-023-40064-9
2407 10145 76 None - 7 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
59227 10145 76 None - 7 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
941 10145 76 None - 7 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
CHEMBL1303 10145 76 None - 7 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
DB05271 10145 76 None - 7 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
3380 29562 34 None - 1 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 2 0 4 2.5 CN1C(=O)CN=C(c2ccccc2F)c2cc([N+](=O)[O-])ccc21 10.1038/s41467-023-40064-9
CHEMBL13280 29562 34 None - 1 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 2 0 4 2.5 CN1C(=O)CN=C(c2ccccc2F)c2cc([N+](=O)[O-])ccc21 10.1038/s41467-023-40064-9
2202 9906 96 None - 21 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
4850 9906 96 None - 21 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
49 9906 96 None - 21 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
CHEMBL1371770 9906 96 None - 21 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
DB12478 9906 96 None - 21 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
4495 203314 92 None - 29 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL56367 203314 92 None - 29 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 10.1038/s41467-023-40064-9
9801 98360 35 None - 0 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 329 8 1 1 5.4 CC(Cc1ccccc1)NCCC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL24072 98360 35 None - 0 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 329 8 1 1 5.4 CC(Cc1ccccc1)NCCC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
6729 21257 41 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 432 5 0 2 6.5 CC(C)(C)c1ccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)cc1 10.1038/s41467-023-40064-9
CHEMBL1201271 21257 41 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 432 5 0 2 6.5 CC(C)(C)c1ccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)cc1 10.1038/s41467-023-40064-9
DB00354 21257 41 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 432 5 0 2 6.5 CC(C)(C)c1ccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)cc1 10.1038/s41467-023-40064-9
1016 10519 78 None - 35 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
2561 10519 78 None - 35 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
2733526 10519 78 None - 35 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
5384 10519 78 None - 35 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL83 10519 78 None - 35 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
DB00675 10519 78 None - 35 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
9915743 70316 93 None - 0 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 556 11 2 8 5.9 CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)/C=C/CN(C)C 10.1038/s41467-023-40064-9
CHEMBL180022 70316 93 None - 0 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 556 11 2 8 5.9 CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)/C=C/CN(C)C 10.1038/s41467-023-40064-9
275196 132451 52 None - 0 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 4 0 8 2.9 COc1ccc2c(c1OC)C(=O)O[C@@H]2[C@H]1c2c(cc3c(c2OC)OCO3)CCN1C 10.1038/s41467-023-40064-9
CHEMBL364713 132451 52 None - 0 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 4 0 8 2.9 COc1ccc2c(c1OC)C(=O)O[C@@H]2[C@H]1c2c(cc3c(c2OC)OCO3)CCN1C 10.1038/s41467-023-40064-9
26987 7736 33 None - 21 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
6063 7736 33 None - 21 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
671 7736 33 None - 21 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
CHEMBL1626 7736 33 None - 21 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
DB00283 7736 33 None - 21 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
11980903 21264 19 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
22526 21264 19 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
5281035 21264 19 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201303 21264 19 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
25077405 9492 0 None - 1 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
3902 9492 0 None - 1 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
49800011 9492 0 None - 1 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
CHEMBL1201309 9492 0 None - 1 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
DB00666 9492 0 None - 1 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
102 10899 48 None - 49 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
3659 10899 48 None - 49 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
8969 10899 48 None - 49 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL15245 10899 48 None - 49 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
DB01392 10899 48 None - 49 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
4034 62596 55 None - 1 Human 4.4 pAC50 = 4.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
CHEMBL1623 62596 55 None - 1 Human 4.4 pAC50 = 4.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
DB00737 62596 55 None - 1 Human 4.4 pAC50 = 4.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
5328940 106992 107 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
CHEMBL288441 106992 107 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
10531 8202 21 None - 24 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
121 8202 21 None - 24 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
888 8202 21 None - 24 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
CHEMBL1732 8202 21 None - 24 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
DB00320 8202 21 None - 24 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
118422671 9533 65 None - 4 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
1887 9533 65 None - 4 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
189562 9533 65 None - 4 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
71301 9533 65 None - 4 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
7246 9533 65 None - 4 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
9844194 9533 65 None - 4 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL2365658 9533 65 None - 4 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL3526436 9533 65 None - 4 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL434394 9533 65 None - 4 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
DB04861 9533 65 None - 4 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
30323 69259 57 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL1563 69259 57 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL178 69259 57 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
10096344 96369 85 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 472 4 1 10 1.1 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(Cc1nc(C)c3ccccc3n1)c(=O)n2C 10.1038/s41467-023-40064-9
CHEMBL237500 96369 85 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 472 4 1 10 1.1 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(Cc1nc(C)c3ccccc3n1)c(=O)n2C 10.1038/s41467-023-40064-9
216416 118358 48 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL328190 118358 48 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
319 8106 44 None - 9 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
321 8106 44 None - 9 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
444031 8106 44 None - 9 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
72054 8106 44 None - 9 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
784 8106 44 None - 9 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
CHEMBL1346 8106 44 None - 9 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
DB00496 8106 44 None - 9 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
3149 19386 15 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1187011 19386 15 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
4746 211670 31 None - 4 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL1334033 211670 31 None - 4 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL75880 211670 31 None - 4 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
2335 18620 22 None - 12 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
8478 18620 22 None - 12 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 18620 22 None - 12 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL221753 18620 22 None - 12 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
65709 66655 39 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 365 8 0 5 3.3 CCN(CC)CCn1c(=O)c(Cc2ccc(OC)cc2)nc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1729803 66655 39 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 365 8 0 5 3.3 CCN(CC)CCn1c(=O)c(Cc2ccc(OC)cc2)nc2ccccc21 10.1038/s41467-023-40064-9
11643449 96730 3 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 753 6 5 10 2.7 CC[C@]1(O)C[C@@H]2CN(CCc3c([nH]c4ccccc34)[C@@](C(=O)OC)(c3cc4c(cc3OC)N(C)[C@H]3[C@@](O)(C(N)=O)[C@H](O)[C@]5(CC)C=CCN6CC[C@]43[C@@H]65)C2)C1 10.1038/s41467-023-40064-9
CHEMBL238071 96730 3 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 753 6 5 10 2.7 CC[C@]1(O)C[C@@H]2CN(CCc3c([nH]c4ccccc34)[C@@](C(=O)OC)(c3cc4c(cc3OC)N(C)[C@H]3[C@@](O)(C(N)=O)[C@H](O)[C@]5(CC)C=CCN6CC[C@]43[C@@H]65)C2)C1 10.1038/s41467-023-40064-9
2448 106099 70 None - 18 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
CHEMBL28218 106099 70 None - 18 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
DB12401 106099 70 None - 18 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
4452 9538 19 None - 18 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
983 9538 19 None - 18 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
CHEMBL20734 9538 19 None - 18 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
176 7186 66 None - 31 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2157 7186 66 None - 31 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2566 7186 66 None - 31 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
CHEMBL633 7186 66 None - 31 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
DB01118 7186 66 None - 31 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
1222 8445 49 None - 32 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3396 8445 49 None - 32 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
85 8445 49 None - 32 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL46516 8445 49 None - 32 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
DB04842 8445 49 None - 32 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
5329102 201505 86 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 201505 86 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
72093 41835 9 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL1433361 41835 9 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL2103773 41835 9 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
42890 16197 59 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 497 3 5 10 1.0 CC(=O)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
CHEMBL1117 16197 59 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 497 3 5 10 1.0 CC(=O)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
1164 8411 26 None - 12 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
1626 8411 26 None - 12 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
3345 8411 26 None - 12 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL596 8411 26 None - 12 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
DB00813 8411 26 None - 12 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
2247 7293 81 None - 42 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 7293 81 None - 42 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 7293 81 None - 42 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 7293 81 None - 42 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 7293 81 None - 42 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
5482 21192 80 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 386 6 0 4 5.9 Clc1ccc(C(Cn2ccnc2)OCc2ccsc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1200438 21192 80 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 386 6 0 4 5.9 Clc1ccc(C(Cn2ccnc2)OCc2ccsc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
1385580 36049 76 None - 5 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
4615 36049 76 None - 5 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL13828 36049 76 None - 5 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
DB12877 36049 76 None - 5 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
16722836 25757 99 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 524 10 3 8 4.8 Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1 10.1038/s41467-023-40064-9
CHEMBL1287853 25757 99 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 524 10 3 8 4.8 Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1 10.1038/s41467-023-40064-9
2794 26152 85 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 472 4 1 4 7.5 CC(C)/N=c1\cc2n(-c3ccc(Cl)cc3)c3ccccc3nc-2cc1Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1292 26152 85 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 472 4 1 4 7.5 CC(C)/N=c1\cc2n(-c3ccc(Cl)cc3)c3ccccc3nc-2cc1Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
3883 190314 112 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 369 5 1 4 3.5 Cc1c(OCC(F)(F)F)ccnc1C[S+]([O-])c1nc2ccccc2[nH]1 10.1038/s41467-023-40064-9
CHEMBL480 190314 112 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 369 5 1 4 3.5 Cc1c(OCC(F)(F)F)ccnc1C[S+]([O-])c1nc2ccccc2[nH]1 10.1038/s41467-023-40064-9
178024 8752 33 None - 1 Human 9.7 pEC50 = 9.7 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm301653f
5867 8752 33 None - 1 Human 9.7 pEC50 = 9.7 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm301653f
CHEMBL13817 8752 33 None - 1 Human 9.7 pEC50 = 9.7 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm301653f
22867441 17087 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
CHEMBL1161835 17087 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
67457995 98608 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@H](O)c1ccccc12 10.1016/j.bmc.2013.06.006
CHEMBL2413152 98608 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@H](O)c1ccccc12 10.1016/j.bmc.2013.06.006
22867441 17087 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
CHEMBL1161835 17087 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
71716660 92777 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 5 5 2.7 CCNC(O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
CHEMBL2304221 92777 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 5 5 2.7 CCNC(O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
10345516 146053 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1021/jm058053k
CHEMBL379074 146053 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1021/jm058053k
71716660 92777 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 5 5 2.7 CCNC(O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
CHEMBL2304221 92777 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 5 5 2.7 CCNC(O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
10345516 146053 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1021/jm058053k
CHEMBL379074 146053 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1021/jm058053k
9807597 189796 5 None - 0 Human 9.0 pEC50 = 9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 513 7 4 4 3.5 CNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1021/jm058053k
CHEMBL47938 189796 5 None - 0 Human 9.0 pEC50 = 9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 513 7 4 4 3.5 CNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1021/jm058053k
10323604 17081 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161828 17081 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
10323604 17081 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161828 17081 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
44411920 84653 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 3 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
CHEMBL209360 84653 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 3 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
162662316 188302 0 None - 0 Rat 8.9 pEC50 = 8.9 Binding
Agonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIAAgonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIA
ChEMBL 542 8 3 6 2.6 CC(C)(N)NC(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CC(S(C)(=O)=O)c1ccccc12 10.1021/acs.jmedchem.0c00829
CHEMBL4765101 188302 0 None - 0 Rat 8.9 pEC50 = 8.9 Binding
Agonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIAAgonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIA
ChEMBL 542 8 3 6 2.6 CC(C)(N)NC(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CC(S(C)(=O)=O)c1ccccc12 10.1021/acs.jmedchem.0c00829
90666017 116077 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at GSH-R1a in human U2OS cells after 2 hrs by FLIPR assayAgonist activity at GSH-R1a in human U2OS cells after 2 hrs by FLIPR assay
ChEMBL 472 6 0 8 4.1 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218890 116077 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at GSH-R1a in human U2OS cells after 2 hrs by FLIPR assayAgonist activity at GSH-R1a in human U2OS cells after 2 hrs by FLIPR assay
ChEMBL 472 6 0 8 4.1 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
44411920 84653 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 3 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
CHEMBL209360 84653 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 3 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
10625750 174933 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
CHEMBL433087 174933 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
10625750 174933 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
CHEMBL433087 174933 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
10626337 108002 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1021/jm058053k
CHEMBL295984 108002 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1021/jm058053k
44411718 17078 0 None - 0 Human 8.0 pEC50 = 8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 467 7 2 5 3.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161825 17078 0 None - 0 Human 8.0 pEC50 = 8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 467 7 2 5 3.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
44293557 107865 0 None - 0 Human 8.0 pEC50 = 8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL294923 107865 0 None - 0 Human 8.0 pEC50 = 8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL540001 107865 0 None - 0 Human 8.0 pEC50 = 8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
16040587 186163 0 None - 0 Human 7.0 pEC50 = 7 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1 10.1021/jm301653f
CHEMBL473921 186163 0 None - 0 Human 7.0 pEC50 = 7 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1 10.1021/jm301653f
16040587 186163 0 None - 0 Human 7.0 pEC50 = 7 Binding
Inhibition of human Ghrelin receptorInhibition of human Ghrelin receptor
ChEMBL 501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1 10.1016/j.bmcl.2008.10.072
CHEMBL473921 186163 0 None - 0 Human 7.0 pEC50 = 7 Binding
Inhibition of human Ghrelin receptorInhibition of human Ghrelin receptor
ChEMBL 501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1 10.1016/j.bmcl.2008.10.072
16752689 195147 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 568 10 2 4 6.6 COc1cccc(CCN(Cc2ccccc2-c2ccc(CN3C[C@H](C)N[C@H](C)C3)cc2)C(=O)NC2CCCCC2)c1 10.1021/jm301653f
CHEMBL501315 195147 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 568 10 2 4 6.6 COc1cccc(CCN(Cc2ccccc2-c2ccc(CN3C[C@H](C)N[C@H](C)C3)cc2)C(=O)NC2CCCCC2)c1 10.1021/jm301653f
9890375 105046 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL274599 105046 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL558802 105046 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
9890375 105046 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL274599 105046 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL558802 105046 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
10026738 169548 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL417182 169548 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL557206 169548 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
10026738 169548 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL417182 169548 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL557206 169548 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
10745533 146898 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL380096 146898 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
10745533 146898 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL380096 146898 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
44411745 17080 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
CHEMBL1161827 17080 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
10626337 108002 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1021/jm058053k
CHEMBL295984 108002 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1021/jm058053k
44411634 17077 1 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161824 17077 1 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
44411634 17077 1 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161824 17077 1 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
44411745 17080 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
CHEMBL1161827 17080 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
44411753 17082 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
CHEMBL1161829 17082 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
44411753 17082 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
CHEMBL1161829 17082 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
44293091 194965 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL49884 194965 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
44293091 194965 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL49884 194965 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
46905972 17181 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 471 10 1 3 4.8 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)Cc1ccccc1 10.1021/jm058053k
CHEMBL1162926 17181 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 471 10 1 3 4.8 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)Cc1ccccc1 10.1021/jm058053k
15481181 84519 2 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
CHEMBL209020 84519 2 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
9810101 106025 17 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL281764 106025 17 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
15481188 147988 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1021/jm058053k
CHEMBL382844 147988 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1021/jm058053k
CHEMBL1793862 215707 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL None None None CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm058053k
216208 16499 33 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIAAgonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIA
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.0c00829
CHEMBL113313 16499 33 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIAAgonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIA
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.0c00829
46905972 17181 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 471 10 1 3 4.8 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)Cc1ccccc1 10.1021/jm058053k
CHEMBL1162926 17181 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 471 10 1 3 4.8 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)Cc1ccccc1 10.1021/jm058053k
15481181 84519 2 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
CHEMBL209020 84519 2 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
9810101 106025 17 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL281764 106025 17 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
15481188 147988 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1021/jm058053k
CHEMBL382844 147988 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1021/jm058053k
CHEMBL1793862 215707 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL None None None CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm058053k
15481185 84036 1 None - 0 Human 8.4 pEC50 = 8.4 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
CHEMBL207970 84036 1 None - 0 Human 8.4 pEC50 = 8.4 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
15481185 84036 1 None - 0 Human 8.4 pEC50 = 8.4 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
CHEMBL207970 84036 1 None - 0 Human 8.4 pEC50 = 8.4 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
44411584 17075 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161822 17075 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
44411584 17075 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161822 17075 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
22862436 17086 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161834 17086 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
10602640 144967 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1021/jm058053k
CHEMBL376970 144967 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1021/jm058053k
10791616 146314 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL379564 146314 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
10029990 176063 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL441360 176063 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
22862436 17086 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161834 17086 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
10602640 144967 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1021/jm058053k
CHEMBL376970 144967 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1021/jm058053k
10791616 146314 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL379564 146314 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
10029990 176063 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL441360 176063 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
44411632 17076 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161823 17076 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
44411632 17076 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161823 17076 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
23529194 108968 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
Agonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIAAgonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIA
ChEMBL 525 5 3 3 4.0 O=C(NC(Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1)NC1CN2CCC1CC2 10.1021/acs.jmedchem.0c00829
CHEMBL302810 108968 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
Agonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIAAgonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIA
ChEMBL 525 5 3 3 4.0 O=C(NC(Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1)NC1CN2CCC1CC2 10.1021/acs.jmedchem.0c00829
16041292 190390 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Inhibition of human Ghrelin receptorInhibition of human Ghrelin receptor
ChEMBL 490 6 2 6 3.9 C[C@H]1CN(Cc2ccc(-n3ccnc3C(=O)N3CCC(Nc4cccc(F)c4)CC3)cc2)C[C@@H](C)N1 10.1016/j.bmcl.2008.10.072
CHEMBL480219 190390 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Inhibition of human Ghrelin receptorInhibition of human Ghrelin receptor
ChEMBL 490 6 2 6 3.9 C[C@H]1CN(Cc2ccc(-n3ccnc3C(=O)N3CCC(Nc4cccc(F)c4)CC3)cc2)C[C@@H](C)N1 10.1016/j.bmcl.2008.10.072
44411913 17085 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161833 17085 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
44411913 17085 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161833 17085 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
44411905 17084 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161832 17084 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
10506325 108018 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1021/jm058053k
CHEMBL296104 108018 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1021/jm058053k
44411905 17084 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161832 17084 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
10506325 108018 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1021/jm058053k
CHEMBL296104 108018 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1021/jm058053k
10600702 148114 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL383526 148114 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
10600702 148114 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL383526 148114 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL335799 218343 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmc.2013.06.006
44411720 17079 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
CHEMBL1161826 17079 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
44411902 17083 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
CHEMBL1161831 17083 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
44411720 17079 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
CHEMBL1161826 17079 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
44411902 17083 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
CHEMBL1161831 17083 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
44390849 69689 0 None - 0 Human 10.7 pIC50 = 10.7 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc(Cl)cc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL178475 69689 0 None - 0 Human 10.7 pIC50 = 10.7 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc(Cl)cc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
25227441 120220 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 563 8 2 8 3.9 CCc1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
CHEMBL3319217 120220 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 563 8 2 8 3.9 CCc1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
CHEMBL501253 220912 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](COC(=O)CCCCCCCBr)NC(=O)[C@H](CO)NC(=O)CN)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm0001727
44582528 200195 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 3419 113 48 48 -14.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](COC(=O)CC12CC3CC(CC(C3)C1)C2)NC(=O)[C@H](CO)NC(=O)CN)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm0001727
91935097 200195 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 3419 113 48 48 -14.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](COC(=O)CC12CC3CC(CC(C3)C1)C2)NC(=O)[C@H](CO)NC(=O)CN)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm0001727
CHEMBL525994 200195 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 3419 113 48 48 -14.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](COC(=O)CC12CC3CC(CC(C3)C1)C2)NC(=O)[C@H](CO)NC(=O)CN)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm0001727
CHEMBL2310891 216274 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C(C)C 10.1021/jm0001727
90665845 116049 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 485 5 0 4 6.8 Cc1ccccc1-c1nc2ccc(-c3ccc(Cl)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218645 116049 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 485 5 0 4 6.8 Cc1ccccc1-c1nc2ccc(-c3ccc(Cl)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL500468 220894 0 None - 1 Human 9.9 pIC50 = 9.9 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/j.bmcl.2005.02.042
57422686 120224 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 600 8 2 9 4.1 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccc5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319221 120224 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 600 8 2 9 4.1 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccc5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL2310888 216272 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(N)=O)C(C)C 10.1021/jm0001727
11340044 148113 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(NCc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL383522 148113 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(NCc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
44336274 115347 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration (biotinylated probe) is evaluated for [35S]- MK-0677 bindingInhibitory concentration (biotinylated probe) is evaluated for [35S]- MK-0677 binding
ChEMBL 896 22 6 10 2.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CN(S(=O)(=O)CC(=O)NCCCCCCNC(=O)CCCC[C@@H]1SCC3NC(=O)NC31)c1ccccc12 10.1021/jm970342o
CHEMBL320289 115347 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration (biotinylated probe) is evaluated for [35S]- MK-0677 bindingInhibitory concentration (biotinylated probe) is evaluated for [35S]- MK-0677 binding
ChEMBL 896 22 6 10 2.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CN(S(=O)(=O)CC(=O)NCCCCCCNC(=O)CCCC[C@@H]1SCC3NC(=O)NC31)c1ccccc12 10.1021/jm970342o
122180027 128366 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 566 8 2 7 5.2 CC(C)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586033 128366 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 566 8 2 7 5.2 CC(C)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
118709502 120249 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 629 8 2 10 3.8 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)c(C#N)cc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319398 120249 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 629 8 2 10 3.8 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)c(C#N)cc4Cl)sc3c2)CC1 10.1021/jm500610n
44390862 70641 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2cc(Cl)ccc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL180349 70641 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2cc(Cl)ccc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
16133832 220110 18 None - 1 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm0001727
CHEMBL425281 220110 18 None - 1 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm0001727
CHEMBL500468 220894 0 None - 1 Human 9.6 pIC50 = 9.6 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/s0960-894x(01)00324-9
90665847 116051 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 475 5 0 6 5.3 Cc1ccccc1-c1nc2cn(-c3ccc(Cl)cc3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218647 116051 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 475 5 0 6 5.3 Cc1ccccc1-c1nc2cn(-c3ccc(Cl)cc3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
122182190 128787 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
CHEMBL3593815 128787 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
57422687 120225 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 604 8 2 9 3.9 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319222 120225 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 604 8 2 9 3.9 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
16114292 103709 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL266063 103709 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
16114292 103709 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
CHEMBL266063 103709 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
11225576 172816 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL425594 172816 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
122182047 128780 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593636 128780 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
11225576 172816 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL425594 172816 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
25260749 120223 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 579 9 2 9 3.7 CCOc1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
CHEMBL3319220 120223 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 579 9 2 9 3.7 CCOc1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
57422792 120248 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 635 8 2 10 4.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)c(Cl)cc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319397 120248 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 635 8 2 10 4.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)c(Cl)cc4Cl)sc3c2)CC1 10.1021/jm500610n
57422692 120222 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 575 8 2 8 4.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(C5CC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319219 120222 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 575 8 2 8 4.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(C5CC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL500468 220894 0 None - 1 Human 9.4 pIC50 = 9.4 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1021/jm020985q
122182043 128776 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 580 7 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593632 128776 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 580 7 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
118709506 120259 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 586 5 2 9 4.3 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)c(C#N)cc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319407 120259 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 586 5 2 9 4.3 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)c(C#N)cc4Cl)sc3c2)CC1 10.1021/jm500610n
178024 8752 33 None - 1 Human 9.4 pIC50 = 9.4 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm0309452
5867 8752 33 None - 1 Human 9.4 pIC50 = 9.4 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm0309452
CHEMBL13817 8752 33 None - 1 Human 9.4 pIC50 = 9.4 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm0309452
11431274 84119 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 467 9 3 8 3.8 CC(C)=CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL208424 84119 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 467 9 3 8 3.8 CC(C)=CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11410373 145313 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 558 10 4 8 4.2 Cc1cc(C)cc(CNC(=O)CCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)c1 10.1016/j.bmcl.2006.01.012
CHEMBL377514 145313 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 558 10 4 8 4.2 Cc1cc(C)cc(CNC(=O)CCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)c1 10.1016/j.bmcl.2006.01.012
44582531 195501 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 3368 117 49 47 -15.3 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm0001727
91935100 195501 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 3368 117 49 47 -15.3 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm0001727
CHEMBL504776 195501 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 3368 117 49 47 -15.3 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm0001727
122182046 128779 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 586 8 2 6 5.6 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCC3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593635 128779 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 586 8 2 6 5.6 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCC3)cc1Cl 10.1016/j.bmc.2015.05.047
25260745 120252 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 573 10 2 8 5.2 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(-n4cccc4)ccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319400 120252 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 573 10 2 8 5.2 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(-n4cccc4)ccc3Cl)sc2c1 10.1021/jm500610n
122182190 128787 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
CHEMBL3593815 128787 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
57422768 120231 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 615 8 2 10 3.8 Cc1ccn(-c2ccc(C(=O)NC(=O)Nc3nc4ccc(S(=O)(=O)CCCN5CCN(C)CC5)cc4s3)c(Cl)c2)n1 10.1021/jm500610n
CHEMBL3319228 120231 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 615 8 2 10 3.8 Cc1ccn(-c2ccc(C(=O)NC(=O)Nc3nc4ccc(S(=O)(=O)CCCN5CCN(C)CC5)cc4s3)c(Cl)c2)n1 10.1021/jm500610n
16114096 85935 1 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)c(OC)c1 10.1021/jm0704550
CHEMBL2113324 85935 1 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)c(OC)c1 10.1021/jm0704550
178024 8752 33 None - 1 Human 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cellsAbility to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cells
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020424z
5867 8752 33 None - 1 Human 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cellsAbility to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cells
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020424z
CHEMBL13817 8752 33 None - 1 Human 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cellsAbility to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cells
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020424z
57422690 120230 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 615 8 2 10 3.8 Cc1ccn(-c2ccc(Cl)c(C(=O)NC(=O)Nc3nc4ccc(S(=O)(=O)CCCN5CCN(C)CC5)cc4s3)c2)n1 10.1021/jm500610n
CHEMBL3319227 120230 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 615 8 2 10 3.8 Cc1ccn(-c2ccc(Cl)c(C(=O)NC(=O)Nc3nc4ccc(S(=O)(=O)CCCN5CCN(C)CC5)cc4s3)c2)n1 10.1021/jm500610n
118709503 120250 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 588 7 2 9 3.8 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc5c(ccn5C)cc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319399 120250 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 588 7 2 9 3.8 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc5c(ccn5C)cc4Cl)sc3c2)CC1 10.1021/jm500610n
66788278 131970 0 None - 1 Human 9.2 pIC50 = 9.2 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 nan
CHEMBL3645254 131970 0 None - 1 Human 9.2 pIC50 = 9.2 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 nan
16114292 103709 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm701292s
CHEMBL266063 103709 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm701292s
44436850 98324 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 564 11 4 6 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL240509 98324 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 564 11 4 6 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
57422793 120247 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 631 9 2 11 3.5 COc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1021/jm500610n
CHEMBL3319396 120247 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 631 9 2 11 3.5 COc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1021/jm500610n
178024 8752 33 None - 1 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(01)00324-9
5867 8752 33 None - 1 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(01)00324-9
CHEMBL13817 8752 33 None - 1 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(01)00324-9
57422688 120228 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 601 8 2 10 3.5 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319225 120228 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 601 8 2 10 3.5 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
57785733 120227 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 612 8 2 9 4.4 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-c5ccccn5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319224 120227 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 612 8 2 9 4.4 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-c5ccccn5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
16113245 128112 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581030 128112 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2014.11.031
44445600 161567 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 542 10 2 6 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL400175 161567 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 542 10 2 6 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL437713 220510 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Ability to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) expressed in COS-7 cellsAbility to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) expressed in COS-7 cells
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C(C)C 10.1021/jm020424z
178024 8752 33 None - 1 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020985q
5867 8752 33 None - 1 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020985q
CHEMBL13817 8752 33 None - 1 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020985q
CHEMBL412799 219804 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(N)=O)C(C)C 10.1021/jm0001727
57422817 120226 18 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 620 8 2 10 3.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319223 120226 18 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 620 8 2 10 3.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
11476589 82763 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(CNc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205451 82763 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(CNc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL526723 222476 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm0001727
44436857 152434 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 594 12 4 7 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL391588 152434 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 594 12 4 7 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
90666039 116099 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 528 8 0 9 4.2 CCOc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218912 116099 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 528 8 0 9 4.2 CCOc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
118709505 120258 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 561 5 2 8 4.4 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319406 120258 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 561 5 2 8 4.4 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL2310887 216271 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCC(CCC)C(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C(C)C 10.1021/jm0001727
122180026 128365 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 566 7 2 7 4.4 CC(=O)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586032 128365 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 566 7 2 7 4.4 CC(=O)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
122182043 128776 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 580 7 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593632 128776 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 580 7 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL2310890 216273 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None C/C=C/C=C/C=C/C(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C(C)C 10.1021/jm0001727
44409536 82284 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 579 9 3 8 5.2 Nc1nc(N)c(-c2ccc(NCc3cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL204325 82284 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 579 9 3 8 5.2 Nc1nc(N)c(-c2ccc(NCc3cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
44445595 101178 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 572 11 2 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL250974 101178 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 572 11 2 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
90665850 116054 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 491 7 0 7 4.6 COCCN1CCC[C@@H](Cn2c(-c3ccccc3C)nc3cn(-c4ccc(Cl)cc4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218650 116054 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 491 7 0 7 4.6 COCCN1CCC[C@@H](Cn2c(-c3ccccc3C)nc3cn(-c4ccc(Cl)cc4)nc3c2=O)C1 10.1039/C2MD20340E
90665851 116055 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 459 5 0 6 4.8 Cc1ccccc1-c1nc2cn(-c3ccc(F)cc3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218651 116055 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 459 5 0 6 4.8 Cc1ccccc1-c1nc2cn(-c3ccc(F)cc3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
11134880 106207 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 500 10 6 4 2.1 O=CN[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCNCC1 10.1021/jm020985q
CHEMBL282891 106207 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 500 10 6 4 2.1 O=CN[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCNCC1 10.1021/jm020985q
5866 10396 4 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 10.1021/jm040103i
9804743 10396 4 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 10.1021/jm040103i
CHEMBL360227 10396 4 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 10.1021/jm040103i
11712151 82768 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 453 9 3 7 4.8 CC(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL205470 82768 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 453 9 3 7 4.8 CC(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
56942098 131971 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 nan
CHEMBL3645255 131971 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 nan
25261382 120218 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 535 7 2 8 3.3 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319215 120218 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 535 7 2 8 3.3 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
57422789 120232 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 629 8 2 10 4.1 Cc1cc(C)n(-c2ccc(Cl)c(C(=O)NC(=O)Nc3nc4ccc(S(=O)(=O)CCCN5CCN(C)CC5)cc4s3)c2)n1 10.1021/jm500610n
CHEMBL3319229 120232 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 629 8 2 10 4.1 Cc1cc(C)n(-c2ccc(Cl)c(C(=O)NC(=O)Nc3nc4ccc(S(=O)(=O)CCCN5CCN(C)CC5)cc4s3)c2)n1 10.1021/jm500610n
56942244 131975 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 nan
CHEMBL3645259 131975 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 nan
90665846 116050 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 491 5 0 5 6.9 Cc1ccccc1-c1nc2cc(-c3ccc(Cl)cc3)sc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218646 116050 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 491 5 0 5 6.9 Cc1ccccc1-c1nc2cc(-c3ccc(Cl)cc3)sc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
11339816 82782 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 446 8 3 7 4.7 Nc1nc(N)c(-c2ccc(NCc3ccnc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205521 82782 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 446 8 3 7 4.7 Nc1nc(N)c(-c2ccc(NCc3ccnc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
44409756 83542 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 492 8 4 8 4.1 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccc(F)cc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206820 83542 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 492 8 4 8 4.1 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccc(F)cc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
90666012 116072 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 475 5 0 6 5.3 Cc1ccccc1-c1nc2cn(-c3cccc(Cl)c3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218885 116072 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 475 5 0 6 5.3 Cc1ccccc1-c1nc2cn(-c3cccc(Cl)c3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
90666031 116091 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 498 7 0 8 4.5 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218904 116091 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 498 7 0 8 4.5 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
44390840 130334 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2cccc(Cl)c2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL361804 130334 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2cccc(Cl)c2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
90666017 116077 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 472 6 0 8 4.1 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218890 116077 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 472 6 0 8 4.1 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
90666027 116087 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 502 8 0 9 3.7 COC[C@H](C)N1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218900 116087 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 502 8 0 9 3.7 COC[C@H](C)N1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
44445594 161421 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 611 11 3 7 6.0 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL399447 161421 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 611 11 3 7 6.0 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
90666013 116073 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 471 6 0 7 4.7 COc1cccc(-n2cc3nc(-c4ccccc4C)n(CC4CCCN(C(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218886 116073 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 471 6 0 7 4.7 COc1cccc(-n2cc3nc(-c4ccccc4C)n(CC4CCCN(C(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
44445599 100959 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 581 10 3 6 6.0 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL249639 100959 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 581 10 3 6 6.0 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
44446187 101396 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252255 101396 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
178024 8752 33 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
5867 8752 33 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
CHEMBL13817 8752 33 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
23648244 98789 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
CHEMBL241775 98789 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
44409776 83918 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 7 3 7 3.5 CC(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL207754 83918 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 7 3 7 3.5 CC(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122178616 128130 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc3ccccc3cn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581048 128130 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc3ccccc3cn2)cc1 10.1016/j.bmcl.2014.11.031
16113471 91496 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 623 10 4 5 6.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(Br)cc1 10.1021/jm070024h
CHEMBL222789 91496 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 623 10 4 5 6.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(Br)cc1 10.1021/jm070024h
156021766 184906 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648355 184906 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145959787 169064 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 169064 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145953855 169294 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4167669 169294 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
16113585 144013 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 591 11 4 7 5.0 COc1ccc(Cn2c(Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
CHEMBL375161 144013 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 591 11 4 7 5.0 COc1ccc(Cn2c(Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
145958774 169045 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163811 169045 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
156016073 184434 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@@H](C)C1 10.1016/j.bmcl.2020.126953
CHEMBL4641503 184434 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@@H](C)C1 10.1016/j.bmcl.2020.126953
162646061 186310 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of GHSR-1A (unknown origin)Inhibition of GHSR-1A (unknown origin)
ChEMBL 729 18 11 12 -5.4 C[C@@H](O)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CN)NC(=O)[C@H](CO)NC(=O)CN)C(N)=O 10.1039/d0md00210k
CHEMBL4741413 186310 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of GHSR-1A (unknown origin)Inhibition of GHSR-1A (unknown origin)
ChEMBL 729 18 11 12 -5.4 C[C@@H](O)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CN)NC(=O)[C@H](CO)NC(=O)CN)C(N)=O 10.1039/d0md00210k
70692600 82649 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 447 7 0 7 2.8 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048813 82649 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 447 7 0 7 2.8 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2310886 216270 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCNC(=O)CCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C(C)C 10.1021/jm0001727
156021766 184906 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648355 184906 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44445601 100960 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 498 8 2 5 5.4 O=C(N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1-c1ccccc1)c1ccccn1 10.1021/jm701292s
CHEMBL249640 100960 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 498 8 2 5 5.4 O=C(N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1-c1ccccc1)c1ccccn1 10.1021/jm701292s
44390901 70853 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 465 8 2 5 2.7 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc(OC)cc2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL180755 70853 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 465 8 2 5 2.7 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc(OC)cc2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
145959787 169064 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 169064 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
70694648 82647 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 462 7 0 7 3.6 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-c4nnc(C)o4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048811 82647 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 462 7 0 7 3.6 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-c4nnc(C)o4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
44445591 161420 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 591 11 4 7 5.0 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)C(C)(C)N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL399446 161420 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 591 11 4 7 5.0 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)C(C)(C)N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
16113468 148578 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
CHEMBL386218 148578 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
16113468 148578 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL386218 148578 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
46882103 12726 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 432 12 4 4 4.1 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCCN)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079872 12726 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 432 12 4 4 4.1 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCCN)cc2)cc1 10.1016/j.bmcl.2009.08.076
72190450 99050 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426679 99050 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
11441978 137233 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 437 8 2 4 4.8 CCN(CC)c1ccc(NC(=O)C2(NC(=O)OCC(C)C)CCc3ccccc3C2)cc1 10.1021/jm0491750
CHEMBL368034 137233 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 437 8 2 4 4.8 CCN(CC)c1ccc(NC(=O)C2(NC(=O)OCC(C)C)CCc3ccccc3C2)cc1 10.1021/jm0491750
CHEMBL2310894 216276 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](COC(=O)c1ccccc1)NC(=O)[C@H](CO)NC(=O)CN)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O 10.1021/jm0001727
122180017 128356 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 525 9 2 8 4.5 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586023 128356 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 525 9 2 8 4.5 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
44445592 100958 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)C(C)(C)N)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL249638 100958 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)C(C)(C)N)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
16113577 91711 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 573 12 4 5 5.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
CHEMBL223725 91711 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 573 12 4 5 5.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
16113902 144454 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL375859 144454 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
90666041 116101 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 542 8 0 9 4.6 Cc1ncccc1-c1nc2cn(-c3cccc(OC(C)C)c3)nc2c(=O)n1C[C@H]1CCCN(C[C@H]2CCCO2)C1 10.1039/C2MD20340E
CHEMBL3218914 116101 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 542 8 0 9 4.6 Cc1ncccc1-c1nc2cn(-c3cccc(OC(C)C)c3)nc2c(=O)n1C[C@H]1CCCN(C[C@H]2CCCO2)C1 10.1039/C2MD20340E
16113902 144454 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL375859 144454 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
15945877 153717 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCCN2)cc1 10.1021/jm0704550
CHEMBL392593 153717 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCCN2)cc1 10.1021/jm0704550
11337482 83415 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
CHEMBL206399 83415 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
44409775 82800 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 8 3 7 3.7 CCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205605 82800 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 8 3 7 3.7 CCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122182190 128787 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Antagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA methodAntagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA method
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
CHEMBL3593815 128787 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Antagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA methodAntagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA method
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
44445620 161457 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 571 11 2 6 6.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccc2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL399651 161457 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 571 11 2 6 6.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccc2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
11676995 72936 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 461 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCOC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL184258 72936 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 461 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCOC)cc1 10.1016/j.bmcl.2004.06.060
16203930 91110 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 552 11 3 7 4.6 COc1cc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc(OC)c1 10.1021/jm070024h
CHEMBL221674 91110 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 552 11 3 7 4.6 COc1cc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc(OC)c1 10.1021/jm070024h
11537683 82302 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 354 5 3 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccnc(Cl)c2)cc1 10.1021/jm0510934
CHEMBL204352 82302 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 354 5 3 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccnc(Cl)c2)cc1 10.1021/jm0510934
122180020 128359 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586026 128359 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
44338247 14699 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 549 11 1 6 4.8 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=O)N1CCCN1CCCC1 10.1016/j.bmcl.2003.11.012
CHEMBL109035 14699 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 549 11 1 6 4.8 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=O)N1CCCN1CCCC1 10.1016/j.bmcl.2003.11.012
44445622 161458 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 625 11 4 7 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccc2N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL399653 161458 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 625 11 4 7 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccc2N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
59446139 88376 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 849 21 10 8 2.2 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163449 88376 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 849 21 10 8 2.2 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44436812 98539 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 11 4 6 3.9 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](C)N)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL241033 98539 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 11 4 6 3.9 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](C)N)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
11731384 169499 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 557 10 7 5 2.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCCCN1 10.1021/jm020985q
CHEMBL417092 169499 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 557 10 7 5 2.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCCCN1 10.1021/jm020985q
44390888 71190 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 435 7 2 4 2.7 CCN(CC)CCN1C(=O)C(O)(c2ccccc2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL181312 71190 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 435 7 2 4 2.7 CCN(CC)CCN1C(=O)C(O)(c2ccccc2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
60195112 88381 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 875 21 10 8 2.6 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163466 88381 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 875 21 10 8 2.6 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2370788 216700 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL None None None Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm020985q
16113904 143814 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 12 3 6 5.1 COc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL374655 143814 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 12 3 6 5.1 COc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
90665852 116056 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 466 5 0 7 4.6 Cc1ccccc1-c1nc2cn(-c3ccc(C#N)cc3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218652 116056 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 466 5 0 7 4.6 Cc1ccccc1-c1nc2cn(-c3ccc(C#N)cc3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
90666032 116092 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 512 7 0 8 4.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218905 116092 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 512 7 0 8 4.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
16113904 143814 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 550 12 3 6 5.1 COc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL374655 143814 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 550 12 3 6 5.1 COc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL500703 220899 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCNC(=N)N)C(N)=O 10.1074/jbc.m609796200
10415364 133545 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against rat Growth hormone secretagogue receptorInhibitory concentration against rat Growth hormone secretagogue receptor
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL365294 133545 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against rat Growth hormone secretagogue receptorInhibitory concentration against rat Growth hormone secretagogue receptor
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
53390181 99046 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN(C2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426675 99046 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN(C2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
145957075 169058 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164040 169058 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
145956026 169441 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4169979 169441 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145956061 169472 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4170481 169472 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
145951150 169555 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4171914 169555 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
11328064 167091 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 437 6 2 4 4.9 CCN(CC)c1ccc(NC(=O)C2(NC(=O)OC(C)(C)C)CCc3ccccc3C2)cc1 10.1021/jm0491750
CHEMBL411055 167091 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 437 6 2 4 4.9 CCN(CC)c1ccc(NC(=O)C2(NC(=O)OC(C)(C)C)CCc3ccccc3C2)cc1 10.1021/jm0491750
44445607 173509 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 572 11 2 7 5.4 COc1ccc(-n2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL428314 173509 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 572 11 2 7 5.4 COc1ccc(-n2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
16113581 91912 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1cccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL224921 91912 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1cccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
90666022 116082 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 528 7 0 9 4.2 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218895 116082 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 528 7 0 9 4.2 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
90666028 116088 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 511 7 0 10 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(Cc5cnco5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218901 116088 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 511 7 0 10 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(Cc5cnco5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
70682036 82653 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 446 7 1 4 4.3 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4n[nH]c5ccccc45)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048817 82653 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 446 7 1 4 4.3 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4n[nH]c5ccccc45)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
16113796 91456 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL222518 91456 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
57422697 120238 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 409 3 2 6 3.3 CS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319276 120238 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 409 3 2 6 3.3 CS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL499371 220874 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCC(N)=O)C(N)=O 10.1074/jbc.m609796200
59446101 88391 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 915 23 11 9 2.1 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163477 88391 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 915 23 11 9 2.1 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
59446101 88391 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 915 23 11 9 2.1 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163477 88391 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 915 23 11 9 2.1 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44389262 128810 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 479 6 2 4 6.1 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccccc1 10.1016/j.bmcl.2004.11.075
CHEMBL359506 128810 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 479 6 2 4 6.1 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccccc1 10.1016/j.bmcl.2004.11.075
16113796 91456 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL222518 91456 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
11576960 73889 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 500 8 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL187427 73889 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 500 8 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
11124146 105929 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 518 10 6 5 2.8 CCOC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL281173 105929 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 518 10 6 5 2.8 CCOC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
122178600 128114 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581033 128114 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2)cc1 10.1016/j.bmcl.2014.11.031
44409679 82283 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 466 8 4 8 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204322 82283 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 466 8 4 8 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
9745 9231 20 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
9804938 9231 20 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
CHEMBL278623 9231 20 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
DB13074 9231 20 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
16113579 91712 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 595 10 4 5 6.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1cccc2ccccc12 10.1021/jm070024h
CHEMBL223726 91712 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 595 10 4 5 6.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1cccc2ccccc12 10.1021/jm070024h
CHEMBL3578015 218545 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
145954311 169265 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4167267 169265 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL3578015 218545 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
11373823 85278 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 431 7 3 7 4.3 Nc1nc(N)c(-c2ccc(NC(=O)c3ccsc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL211188 85278 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 431 7 3 7 4.3 Nc1nc(N)c(-c2ccc(NC(=O)c3ccsc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
145954311 169265 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4167267 169265 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
44301389 18047 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1179118 18047 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL61292 18047 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
46882236 12544 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 8 4 4 4.1 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078608 12544 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 8 4 4 4.1 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
16114514 85933 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCCNC1 10.1021/jm0704550
CHEMBL2113322 85933 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCCNC1 10.1021/jm0704550
11523411 82330 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 363 6 4 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)O)cc2)cc1 10.1021/jm0510934
CHEMBL204511 82330 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 363 6 4 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)O)cc2)cc1 10.1021/jm0510934
57422730 120215 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 508 9 2 7 4.4 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319212 120215 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 508 9 2 7 4.4 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
46882763 12400 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [35S]MK0677 from human GHS-R1aDisplacement of [35S]MK0677 from human GHS-R1a
ChEMBL 612 17 6 7 5.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1077617 12400 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [35S]MK0677 from human GHS-R1aDisplacement of [35S]MK0677 from human GHS-R1a
ChEMBL 612 17 6 7 5.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
44576247 221001 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 221001 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
145951150 169555 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4171914 169555 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL433540 220421 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Ability to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) expressed in COS-7 cellsAbility to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) expressed in COS-7 cells
ChEMBL None None None C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm020424z
1744826 69772 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1021/jm0491750
CHEMBL178668 69772 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1021/jm0491750
1744826 69772 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Binding affinity to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL178668 69772 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Binding affinity to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.06.060
122178603 128117 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 590 11 2 6 6.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(Cl)nc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581036 128117 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 590 11 2 6 6.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(Cl)nc2)cc1 10.1016/j.bmcl.2014.11.031
16114009 143972 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 556 10 3 5 5.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1cccc2ccccc12 10.1021/jm070024h
CHEMBL374921 143972 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 556 10 3 5 5.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1cccc2ccccc12 10.1021/jm070024h
23648246 168567 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 560 11 3 5 5.6 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
CHEMBL414132 168567 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 560 11 3 5 5.6 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
11655578 176812 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 462 8 3 7 5.2 Nc1nc(N)c(-c2ccc(NCc3cnc4ccccc4c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL444277 176812 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 462 8 3 7 5.2 Nc1nc(N)c(-c2ccc(NCc3cnc4ccccc4c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
1744826 69772 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178668 69772 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
156021336 184946 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 467 5 1 6 5.2 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccccc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4649089 184946 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 467 5 1 6 5.2 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccccc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
44446190 101331 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL251855 101331 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
44389167 130636 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 425 7 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL362612 130636 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 425 7 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44338240 115916 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 569 11 1 7 5.2 O=C1[C@H](CCc2ccccc2)N(Cc2cc(-c3ccccc3-c3nn[nH]n3)cs2)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
CHEMBL321403 115916 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 569 11 1 7 5.2 O=C1[C@H](CCc2ccccc2)N(Cc2cc(-c3ccccc3-c3nn[nH]n3)cs2)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
11539587 73851 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 445 8 1 4 6.7 CCCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL187271 73851 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 445 8 1 4 6.7 CCCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
11503585 71978 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 461 9 2 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCCO)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL182542 71978 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 461 9 2 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCCO)cc1 10.1016/j.bmcl.2004.06.060
23656300 155545 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 592 12 3 7 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2)c(OC)c1 10.1021/jm0704550
CHEMBL394054 155545 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 592 12 3 7 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2)c(OC)c1 10.1021/jm0704550
59446107 88394 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163480 88394 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
59446107 88394 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163480 88394 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44436807 155090 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 547 11 3 7 4.6 COc1ccc(Cn2c(CCC3C=Nc4ccccc43)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/jm0704550
CHEMBL393692 155090 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 547 11 3 7 4.6 COc1ccc(Cn2c(CCC3C=Nc4ccccc43)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/jm0704550
46882237 12552 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 466 9 4 4 4.1 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NCCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078677 12552 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 466 9 4 4 4.1 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NCCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
44395002 72960 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 534 9 1 5 5.6 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL184368 72960 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 534 9 1 5 5.6 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)CC1 10.1016/j.bmcl.2004.06.060
44445627 161719 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 543 10 2 7 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL401084 161719 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 543 10 2 7 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
16113906 144001 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 612 12 5 5 6.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
CHEMBL375102 144001 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 612 12 5 5 6.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
70692601 82650 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 481 7 0 7 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048814 82650 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 481 7 0 7 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
145957075 169058 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164040 169058 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
145956026 169441 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4169979 169441 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145956061 169472 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4170481 169472 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
46882271 12581 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 466 8 4 4 5.0 CCc1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078899 12581 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 466 8 4 4 5.0 CCc1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
156018364 184692 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645148 184692 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44445624 161685 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 631 11 4 7 5.8 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)[C@H]2CCCC[C@H]2N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL400879 161685 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 631 11 4 7 5.8 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)[C@H]2CCCC[C@H]2N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
16203238 143887 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 531 9 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1 10.1021/jm070024h
CHEMBL374757 143887 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 531 9 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1 10.1021/jm070024h
16113694 143971 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 609 11 4 5 6.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1cccc2ccccc12 10.1021/jm070024h
CHEMBL374920 143971 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 609 11 4 5 6.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1cccc2ccccc12 10.1021/jm070024h
16114181 148718 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 520 10 3 5 5.0 Cc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL387109 148718 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 520 10 3 5 5.0 Cc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
44446137 162196 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL403682 162196 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
122180017 128356 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 525 9 2 8 4.5 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586023 128356 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 525 9 2 8 4.5 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
44379072 19570 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 492 8 2 5 4.2 NCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1188124 19570 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 492 8 2 5 4.2 NCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL535353 19570 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 492 8 2 5 4.2 NCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
16113905 91472 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 589 12 4 6 5.6 COc1ccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL222622 91472 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 589 12 4 6 5.6 COc1ccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
11626181 131159 2 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 431 7 1 4 6.3 CCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL363896 131159 2 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 431 7 1 4 6.3 CCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
42624369 195642 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1713 58 25 24 -9.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
44582535 195642 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1713 58 25 24 -9.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
91935102 195642 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1713 58 25 24 -9.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
CHEMBL506930 195642 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1713 58 25 24 -9.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
16113691 143497 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
CHEMBL374073 143497 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
90666023 116083 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218896 116083 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
16113691 143497 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm0704550
CHEMBL374073 143497 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm0704550
57422696 120255 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 558 5 2 9 4.0 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319403 120255 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 558 5 2 9 4.0 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
156012849 184077 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4636571 184077 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44390860 70418 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CC)CCN1C(=O)[C@@](O)(c2cccc(Cl)c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL180096 70418 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CC)CCN1C(=O)[C@@](O)(c2cccc(Cl)c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
73347725 99045 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 476 6 0 5 4.5 COc1ccc(CC(=O)N2CCC3(CC2)CN(Cc2ccc(-c4ncccn4)cc2Cl)C3)cc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426674 99045 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 476 6 0 5 4.5 COc1ccc(CC(=O)N2CCC3(CC2)CN(Cc2ccc(-c4ncccn4)cc2Cl)C3)cc1 10.1016/j.bmcl.2013.07.044
156012849 184077 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4636571 184077 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156015928 184360 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4640615 184360 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156018364 184692 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645148 184692 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145949595 169503 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4171040 169503 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
1100 8389 45 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None None 10.1021/jm300557t
6918297 8389 45 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None None 10.1021/jm300557t
CHEMBL108335 8389 45 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None None 10.1021/jm300557t
11539588 73687 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 445 7 1 4 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C(C)C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL186540 73687 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 445 7 1 4 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C(C)C)cc1 10.1016/j.bmcl.2004.06.060
122180015 128354 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 523 9 2 8 5.3 CCCn1cc(-c2cnc(NCc3ccc4occc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586021 128354 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 523 9 2 8 5.3 CCCn1cc(-c2cnc(NCc3ccc4occc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
122178615 128082 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2nccc3ccccc23)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3580668 128082 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2nccc3ccccc23)cc1 10.1016/j.bmcl.2014.11.031
16113798 91108 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 598 11 5 5 5.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
CHEMBL221662 91108 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 598 11 5 5 5.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
16113797 144915 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 637 11 4 5 6.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1ccc(Br)cc1 10.1021/jm070024h
CHEMBL376735 144915 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 637 11 4 5 6.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1ccc(Br)cc1 10.1021/jm070024h
16113903 175156 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1cc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc(OC)c1 10.1021/jm070024h
CHEMBL434573 175156 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1cc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc(OC)c1 10.1021/jm070024h
44338241 13313 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 569 11 1 7 5.2 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)s2)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
CHEMBL108287 13313 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 569 11 1 7 5.2 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)s2)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
44410012 145177 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 439 9 3 7 4.1 CCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL377305 145177 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 439 9 3 7 4.1 CCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
16113122 154947 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 538 12 3 7 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)c(OC)c1 10.1021/jm0704550
CHEMBL393565 154947 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 538 12 3 7 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)c(OC)c1 10.1021/jm0704550
11556937 88397 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163484 88397 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
11556937 88397 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163484 88397 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
9956908 19868 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 482 12 2 5 4.5 NCCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1190326 19868 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 482 12 2 5 4.5 NCCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL540604 19868 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 482 12 2 5 4.5 NCCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
11329138 71234 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 481 9 1 5 5.1 CCN(CC)c1ccc(NC(=O)C2(N(C)C(=O)OCC(C)C)CCc3cccc(OC)c3C2)cc1 10.1021/jm0491750
CHEMBL181350 71234 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 481 9 1 5 5.1 CCN(CC)c1ccc(NC(=O)C2(N(C)C(=O)OCC(C)C)CCc3cccc(OC)c3C2)cc1 10.1021/jm0491750
90665848 116052 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 507 7 0 6 6.1 COCCN1CCC[C@@H](Cn2c(-c3ccccc3C)nc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218648 116052 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 507 7 0 6 6.1 COCCN1CCC[C@@H](Cn2c(-c3ccccc3C)nc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1 10.1039/C2MD20340E
23648245 98790 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
CHEMBL241776 98790 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
145949595 169503 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4171040 169503 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
11846625 84659 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 498 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(-c1ccccc1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
CHEMBL209394 84659 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 498 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(-c1ccccc1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
44409683 83034 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 480 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205848 83034 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 480 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
46882305 12600 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 494 7 4 4 5.7 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)Nc3ccc(C(C)(C)C)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079091 12600 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 494 7 4 4 5.7 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)Nc3ccc(C(C)(C)C)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
11124146 105929 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 518 10 6 5 2.8 CCOC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL281173 105929 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 518 10 6 5 2.8 CCOC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
56942855 131977 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 601 10 2 6 7.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2ccc3ccccc3c2)NC(=O)OC(C)(C)C)cc1 nan
CHEMBL3645261 131977 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 601 10 2 6 7.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2ccc3ccccc3c2)NC(=O)OC(C)(C)C)cc1 nan
11016748 105126 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 517 10 7 4 2.4 CCNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL275141 105126 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 517 10 7 4 2.4 CCNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
44445602 100961 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 537 8 3 5 5.9 O=C(N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1)c1ccccn1 10.1021/jm701292s
CHEMBL249659 100961 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 537 8 3 5 5.9 O=C(N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1)c1ccccn1 10.1021/jm701292s
11256439 82154 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 344 5 3 6 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C#N)cc2)cc1 10.1021/jm0510934
CHEMBL203843 82154 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 344 5 3 6 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C#N)cc2)cc1 10.1021/jm0510934
44390881 72877 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 465 8 2 5 2.7 CCN(CC)CCN1C(=O)[C@@](O)(c2ccccc2OC)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL183916 72877 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 465 8 2 5 2.7 CCN(CC)CCN1C(=O)[C@@](O)(c2ccccc2OC)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
44338151 116526 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 581 11 1 6 5.3 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2F)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
CHEMBL323026 116526 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 581 11 1 6 5.3 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2F)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
46882238 12555 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 7 4 4 4.7 Cc1ccccc1NC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078699 12555 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 7 4 4 4.7 Cc1ccccc1NC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
59446133 181813 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)N(Cc1ccccc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4567432 181813 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)N(Cc1ccccc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
60195284 88385 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)N(Cc1ccccc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163471 88385 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)N(Cc1ccccc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44394930 73106 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2cccc3c2OCO3)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL185028 73106 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2cccc3c2OCO3)cc1 10.1016/j.bmcl.2004.06.060
11016748 105126 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 517 10 7 4 2.4 CCNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL275141 105126 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 517 10 7 4 2.4 CCNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
59446115 181089 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)N(Cc1ccc(-c2ccccc2)cc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4550305 181089 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)N(Cc1ccc(-c2ccccc2)cc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
60195379 88389 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)N(Cc1ccc(-c2ccccc2)cc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163475 88389 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)N(Cc1ccc(-c2ccccc2)cc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
46882155 12480 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 404 8 4 4 3.3 CCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078114 12480 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 404 8 4 4 3.3 CCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
11145720 74114 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 516 11 6 4 2.9 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)NC 10.1021/jm020985q
CHEMBL18853 74114 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 516 11 6 4 2.9 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)NC 10.1021/jm020985q
11846628 84487 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 431 7 2 6 4.2 CN(C(=O)C1CCCC1)c1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
CHEMBL208930 84487 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 431 7 2 6 4.2 CN(C(=O)C1CCCC1)c1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
156015928 184360 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4640615 184360 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
16114012 175178 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 510 9 3 5 4.7 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1ccc(F)cc1 10.1021/jm070024h
CHEMBL434738 175178 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 510 9 3 5 4.7 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1ccc(F)cc1 10.1021/jm070024h
122180018 128357 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 527 9 2 9 4.3 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586024 128357 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 527 9 2 9 4.3 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
16113582 143417 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 455 7 4 5 3.5 Cn1c(Cc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL373995 143417 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 455 7 4 5 3.5 Cn1c(Cc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
46882807 12536 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 404 10 4 4 3.6 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CN)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078533 12536 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 404 10 4 4 3.6 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CN)cc2)cc1 10.1016/j.bmcl.2009.08.076
16114184 157270 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 564 11 4 7 3.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@@H](O)CN2)cc1 10.1021/jm0704550
CHEMBL395441 157270 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 564 11 4 7 3.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@@H](O)CN2)cc1 10.1021/jm0704550
44446188 162170 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL403542 162170 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
44436817 173548 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 600 13 4 6 5.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](N)Cc3ccccc3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL428383 173548 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 600 13 4 6 5.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](N)Cc3ccccc3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44445618 168677 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 570 12 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)CCc2cccnc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL415134 168677 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 570 12 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)CCc2cccnc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
44436887 97734 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 563 11 5 6 3.7 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL239464 97734 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 563 11 5 6 3.7 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
10907396 105926 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 515 10 7 5 1.2 NC1(C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2c[nH]c3ccccc23)NC=O)CCNCC1 10.1021/jm020985q
CHEMBL281147 105926 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 515 10 7 5 1.2 NC1(C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2c[nH]c3ccccc23)NC=O)CCNCC1 10.1021/jm020985q
11649239 73114 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 514 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL185057 73114 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 514 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
1100 8389 45 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL None None None None 10.1021/jm020985q
6918297 8389 45 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL None None None None 10.1021/jm020985q
CHEMBL108335 8389 45 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL None None None None 10.1021/jm020985q
16113580 144657 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm701292s
CHEMBL376258 144657 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm701292s
16113580 144657 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL376258 144657 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
44436883 152931 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 604 11 6 7 3.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2c[nH]c3ccccc23)cc1 10.1021/jm0704550
CHEMBL391980 152931 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 604 11 6 7 3.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2c[nH]c3ccccc23)cc1 10.1021/jm0704550
44436889 159836 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 563 11 3 5 6.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCCCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL397594 159836 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 563 11 3 5 6.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCCCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
11452801 146076 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 417 7 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)C3CCCC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL379191 146076 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 417 7 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)C3CCCC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
44445625 161598 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 612 11 3 8 5.4 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL400381 161598 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 612 11 3 8 5.4 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
122180019 128358 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586025 128358 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
145957443 168868 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
CHEMBL4160928 168868 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
10864048 105164 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.6 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL275373 105164 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.6 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
44389187 70796 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3cccc(Cl)c3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL180722 70796 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3cccc(Cl)c3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44409871 82171 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 426 7 3 8 2.4 CN(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203948 82171 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 426 7 3 8 2.4 CN(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145959007 169036 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163623 169036 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
145956659 168834 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4160434 168834 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
145959787 169064 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 169064 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
16113248 85939 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 560 11 3 5 5.6 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
CHEMBL2113328 85939 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 560 11 3 5 5.6 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
11282247 172705 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL425048 172705 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
11282247 172705 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL425048 172705 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
44409802 83519 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 439 9 3 7 4.1 CCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206687 83519 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 439 9 3 7 4.1 CCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
156019457 184721 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645625 184721 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
216208 16499 33 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
CHEMBL113313 16499 33 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
90666037 116097 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 484 6 0 8 3.8 Cc1ncccc1-c1nc2cn(-c3ccccc3)nc2c(=O)n1C[C@H]1CCCN(C[C@H]2CCCO2)C1 10.1039/C2MD20340E
CHEMBL3218910 116097 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 484 6 0 8 3.8 Cc1ncccc1-c1nc2cn(-c3ccccc3)nc2c(=O)n1C[C@H]1CCCN(C[C@H]2CCCO2)C1 10.1039/C2MD20340E
23648236 85927 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 13 3 7 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NCCN)c(OC)c1 10.1021/jm0704550
CHEMBL2113317 85927 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 13 3 7 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NCCN)c(OC)c1 10.1021/jm0704550
44383343 127120 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 606 6 2 5 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3Cc4ccccc4CN3)CC2)c2ccccc21 10.1021/jm0309452
CHEMBL353007 127120 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 606 6 2 5 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3Cc4ccccc4CN3)CC2)c2ccccc21 10.1021/jm0309452
156014693 183971 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 530 6 2 8 2.9 CCOc1cc(Cl)c(-c2ccc(-c3nc4c(s3)CN(C(=O)CO)CC4)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4635089 183971 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 530 6 2 8 2.9 CCOc1cc(Cl)c(-c2ccc(-c3nc4c(s3)CN(C(=O)CO)CC4)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
44389151 69279 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 445 6 1 4 5.7 CCN(CC)C(=O)c1ccccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
CHEMBL178138 69279 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 445 6 1 4 5.7 CCN(CC)C(=O)c1ccccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
44409979 147337 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 7 2 7 3.4 CCc1nc(N)nc(N(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL381159 147337 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 7 2 7 3.4 CCc1nc(N)nc(N(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44395020 130810 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 507 9 1 5 6.1 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL363021 130810 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 507 9 1 5 6.1 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)CC1 10.1016/j.bmcl.2004.06.060
16114530 91515 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 539 13 4 5 5.7 CCCCCCn1c(CCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL222912 91515 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 539 13 4 5 5.7 CCCCCCn1c(CCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
59446130 88393 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 800 21 10 9 0.4 CC(C)CN(NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163479 88393 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 800 21 10 9 0.4 CC(C)CN(NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
59446130 88393 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 800 21 10 9 0.4 CC(C)CN(NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163479 88393 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 800 21 10 9 0.4 CC(C)CN(NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44409761 82641 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 9 3 7 4.4 CCc1nc(N)nc(NCC(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204880 82641 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 9 3 7 4.4 CCc1nc(N)nc(NCC(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145956659 168834 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4160434 168834 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
145957443 168868 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
CHEMBL4160928 168868 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
145959007 169036 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163623 169036 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
145959787 169064 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 169064 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
11328920 150820 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 471 8 2 4 5.4 CCN(CC)c1ccc(NC(=O)C2(NC(=O)OCC(C)C)CCc3cccc(Cl)c3C2)cc1 10.1021/jm0491750
CHEMBL390308 150820 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 471 8 2 4 5.4 CCN(CC)c1ccc(NC(=O)C2(NC(=O)OCC(C)C)CCc3cccc(Cl)c3C2)cc1 10.1021/jm0491750
122178606 128120 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(F)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581039 128120 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(F)n2)cc1 10.1016/j.bmcl.2014.11.031
122178609 128124 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 586 12 2 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(OC)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581042 128124 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 586 12 2 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(OC)n2)cc1 10.1016/j.bmcl.2014.11.031
178024 8752 33 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
5867 8752 33 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
CHEMBL13817 8752 33 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
44409821 82812 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 564 10 4 8 4.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CCC(=O)NCc3cccc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205711 82812 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 564 10 4 8 4.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CCC(=O)NCc3cccc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2006.01.012
46882307 12602 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 530 8 4 4 6.0 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NC(C)(C)c3cccc4ccccc34)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079108 12602 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 530 8 4 4 6.0 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NC(C)(C)c3cccc4ccccc34)cc2)cc1 10.1016/j.bmcl.2009.08.076
122182044 128777 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 552 9 2 6 4.9 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593633 128777 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 552 9 2 6 4.9 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
5866 10396 4 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 10.1016/j.bmcl.2005.02.042
9804743 10396 4 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 10.1016/j.bmcl.2005.02.042
CHEMBL360227 10396 4 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 10.1016/j.bmcl.2005.02.042
CHEMBL500468 220894 0 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1021/jm501702q
CHEMBL500468 220894 0 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1021/jm501702q
11683469 83481 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 433 6 3 7 3.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(C)(=O)=O)c(F)c2)cc1 10.1021/jm0510934
CHEMBL206486 83481 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 433 6 3 7 3.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(C)(=O)=O)c(F)c2)cc1 10.1021/jm0510934
11454617 148097 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 488 8 3 8 4.0 CN(Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2006.01.012
CHEMBL383411 148097 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 488 8 3 8 4.0 CN(Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2006.01.012
90666029 116089 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 510 7 0 9 4.5 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(Cc5ccco5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218902 116089 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 510 7 0 9 4.5 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(Cc5ccco5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
44409672 147265 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 479 9 3 9 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccco3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL380971 147265 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 479 9 3 9 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccco3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11154823 82804 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 436 8 3 7 4.5 N#Cc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL205660 82804 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 436 8 3 7 4.5 N#Cc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
11190594 82760 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 469 10 3 8 3.9 CC(C)CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205445 82760 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 469 10 3 8 3.9 CC(C)CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11583811 82762 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 479 8 3 6 5.7 Nc1nc(N)c(-c2ccc(NCc3ccc(C(F)(F)F)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205450 82762 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 479 8 3 6 5.7 Nc1nc(N)c(-c2ccc(NCc3ccc(C(F)(F)F)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
25260900 120254 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 593 10 2 9 4.3 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(N4CCOCC4)ccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319402 120254 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 593 10 2 9 4.3 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(N4CCOCC4)ccc3Cl)sc2c1 10.1021/jm500610n
10918326 105748 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N(C)C 10.1021/jm020985q
CHEMBL279822 105748 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N(C)C 10.1021/jm020985q
44378981 20742 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 504 10 2 5 5.5 NCCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1196773 20742 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 504 10 2 5 5.5 NCCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL558181 20742 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 504 10 2 5 5.5 NCCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
90666033 116093 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 526 7 0 8 5.3 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCCC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218906 116093 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 526 7 0 8 5.3 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCCC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
16113472 175785 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2ccccc2)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL439251 175785 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2ccccc2)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
66813470 83607 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]ghrelin from GHS receptorDisplacement of [125I]ghrelin from GHS receptor
ChEMBL 459 6 2 6 3.3 O=C(N[C@@H]1COc2cccc(-c3ccc(CO)nc3)c2C1)c1ccc(OCC(F)(F)F)nc1 10.1016/j.bmcl.2012.06.105
CHEMBL2069411 83607 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]ghrelin from GHS receptorDisplacement of [125I]ghrelin from GHS receptor
ChEMBL 459 6 2 6 3.3 O=C(N[C@@H]1COc2cccc(-c3ccc(CO)nc3)c2C1)c1ccc(OCC(F)(F)F)nc1 10.1016/j.bmcl.2012.06.105
122180022 128361 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 504 7 2 9 2.8 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2CCOCC2)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
CHEMBL3586028 128361 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 504 7 2 9 2.8 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2CCOCC2)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
70694649 82659 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 475 5 0 7 3.2 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-n3nccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
CHEMBL2048823 82659 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 475 5 0 7 3.2 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-n3nccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
10100708 18806 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 530 9 3 7 0.3 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@@H](N)CO)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL1183387 18806 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 530 9 3 7 0.3 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@@H](N)CO)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL294408 18806 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 530 9 3 7 0.3 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@@H](N)CO)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
11577349 72005 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 529 9 1 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCN(C)C2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL182655 72005 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 529 9 1 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCN(C)C2=O)cc1 10.1016/j.bmcl.2004.06.060
16114098 148389 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 534 11 3 5 5.4 Cc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL385131 148389 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 534 11 3 5 5.4 Cc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
11327400 82147 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 412 8 3 7 4.0 Nc1nc(N)c(-c2ccc(NCc3ccncc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL203782 82147 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 412 8 3 7 4.0 Nc1nc(N)c(-c2ccc(NCc3ccncc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
44409455 82743 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 487 6 3 7 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c2)cc1 10.1021/jm0510934
CHEMBL205286 82743 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 487 6 3 7 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c2)cc1 10.1021/jm0510934
156019457 184721 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645625 184721 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
46882306 12601 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 502 8 4 4 5.2 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NCc3cccc4ccccc34)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079107 12601 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 502 8 4 4 5.2 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NCc3cccc4ccccc34)cc2)cc1 10.1016/j.bmcl.2009.08.076
11731384 169499 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 557 10 7 5 2.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCCCN1 10.1021/jm020985q
CHEMBL417092 169499 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 557 10 7 5 2.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCCCN1 10.1021/jm020985q
118709470 120236 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 395 3 2 5 4.6 COc1ccc2nc(NC(=O)NC(=O)c3c(Cl)cccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319274 120236 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 395 3 2 5 4.6 COc1ccc2nc(NC(=O)NC(=O)c3c(Cl)cccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL507636 221212 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H]1CCCN1C(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1074/jbc.m609796200
156021885 184994 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 635 10 1 10 4.2 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1CCO[C@H](C)C1 10.1016/j.bmcl.2020.126953
CHEMBL4649741 184994 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 635 10 1 10 4.2 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1CCO[C@H](C)C1 10.1016/j.bmcl.2020.126953
70688404 82642 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048807 82642 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1016/j.bmcl.2012.05.024
11114279 105025 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 544 12 6 4 3.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(C)C 10.1021/jm020985q
CHEMBL274460 105025 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 544 12 6 4 3.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(C)C 10.1021/jm020985q
70688404 82642 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1016/j.bmcl.2013.07.044
CHEMBL2048807 82642 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1016/j.bmcl.2013.07.044
16113693 144794 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 589 12 4 6 5.6 COc1cccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL376471 144794 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 589 12 4 6 5.6 COc1cccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
216208 16499 33 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
CHEMBL113313 16499 33 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
11827047 105996 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 488 11 6 4 2.1 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC=O 10.1021/jm020985q
CHEMBL281578 105996 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 488 11 6 4 2.1 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC=O 10.1021/jm020985q
9745 9231 20 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
9804938 9231 20 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
CHEMBL278623 9231 20 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
DB13074 9231 20 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
16113124 128113 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccncc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581032 128113 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccncc2)cc1 10.1016/j.bmcl.2014.11.031
44445605 161760 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 542 10 2 6 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccncc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL401260 161760 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 542 10 2 6 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccncc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
16113578 143970 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 542 9 3 5 5.7 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1cccc2ccccc12 10.1021/jm070024h
CHEMBL374919 143970 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 542 9 3 5 5.7 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1cccc2ccccc12 10.1021/jm070024h
16113584 144372 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 441 7 5 4 3.5 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2c[nH]c3ccccc23)[nH]1 10.1021/jm070024h
CHEMBL375568 144372 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 441 7 5 4 3.5 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2c[nH]c3ccccc23)[nH]1 10.1021/jm070024h
44389168 71647 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 457 4 1 4 5.8 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCC1 10.1016/j.bmcl.2004.11.075
CHEMBL182154 71647 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 457 4 1 4 5.8 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCC1 10.1016/j.bmcl.2004.11.075
11314908 148590 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 377 7 3 6 3.4 CCC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
CHEMBL386290 148590 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 377 7 3 6 3.4 CCC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
11846627 86499 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 363 6 3 6 3.0 CC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
CHEMBL211581 86499 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 363 6 3 6 3.0 CC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
10929048 75582 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 488 9 6 4 2.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL19220 75582 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 488 9 6 4 2.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
90666020 116080 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 500 7 0 9 3.5 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218893 116080 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 500 7 0 9 3.5 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
16114403 153965 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2)cc1 10.1021/jm0704550
CHEMBL392805 153965 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2)cc1 10.1021/jm0704550
57422673 120243 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 474 4 2 7 4.1 CS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(-n4cccc4)ccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319282 120243 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 474 4 2 7 4.1 CS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(-n4cccc4)ccc3Cl)sc2c1 10.1021/jm500610n
70684154 82644 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 414 6 0 4 3.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccccc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048809 82644 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 414 6 0 4 3.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccccc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
122180020 128359 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586026 128359 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
16113710 85936 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCNCC1 10.1021/jm0704550
CHEMBL2113325 85936 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCNCC1 10.1021/jm0704550
122178611 128126 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 572 11 3 7 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2O)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581044 128126 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 572 11 3 7 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2O)cc1 10.1016/j.bmcl.2014.11.031
122178614 128129 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 660 13 2 7 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2C(=O)c2ccccc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581047 128129 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 660 13 2 7 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2C(=O)c2ccccc2)cc1 10.1016/j.bmcl.2014.11.031
16114531 91450 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 553 14 4 5 6.1 CCCCCCn1c(CCCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL222498 91450 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 553 14 4 5 6.1 CCCCCCn1c(CCCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
145974293 169803 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4175823 169803 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
46882197 12514 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 432 10 4 4 4.1 CCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078403 12514 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 432 10 4 4 4.1 CCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
44409980 82955 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 8 3 7 3.7 CCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205790 82955 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 8 3 7 3.7 CCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145952740 169280 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4167481 169280 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
44409868 83517 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 487 9 3 7 4.9 CCc1nc(N)nc(NCc2ccccc2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206673 83517 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 487 9 3 7 4.9 CCc1nc(N)nc(NCc2ccccc2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
156017532 184687 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645072 184687 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
11605822 131166 1 None - 0 Human 7.6 pIC50 = 7.6 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 503 9 1 6 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL363930 131166 1 None - 0 Human 7.6 pIC50 = 7.6 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 503 9 1 6 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCO2)cc1 10.1016/j.bmcl.2004.06.060
162651761 186988 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting methodDisplacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting method
ChEMBL 798 19 7 8 3.0 NCCCC[C@H](NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)C(N)=O 10.1016/j.ejmech.2016.07.078
CHEMBL4749698 186988 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting methodDisplacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting method
ChEMBL 798 19 7 8 3.0 NCCCC[C@H](NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)C(N)=O 10.1016/j.ejmech.2016.07.078
70686292 82655 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 461 5 0 8 3.0 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048819 82655 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 461 5 0 8 3.0 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
10186158 105218 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
CHEMBL275660 105218 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
122178602 128116 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2Br)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581035 128116 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2Br)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3586019 218580 6 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CCCNC(=N)N)C(N)=O 10.1016/j.bmcl.2015.04.040
122180025 128364 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 542 7 2 8 3.6 CC(=O)N1CC=C(c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)CC1 10.1016/j.bmcl.2015.04.040
CHEMBL3586031 128364 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 542 7 2 8 3.6 CC(=O)N1CC=C(c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)CC1 10.1016/j.bmcl.2015.04.040
156017532 184687 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645072 184687 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145952740 169280 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4167481 169280 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
145974293 169803 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4175823 169803 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
44436881 98363 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 540 10 4 6 4.6 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1Cc1cccs1)C1CCNCC1 10.1021/jm0704550
CHEMBL240746 98363 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 540 10 4 6 4.6 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1Cc1cccs1)C1CCNCC1 10.1021/jm0704550
122182189 128786 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593814 128786 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
122180016 128355 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 540 9 2 9 5.1 CCCn1cc(-c2cnc(NCc3ccc4ncsc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586022 128355 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 540 9 2 9 5.1 CCCn1cc(-c2cnc(NCc3ccc4ncsc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
46882199 12533 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 438 7 4 4 4.4 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)Nc3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078498 12533 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 438 7 4 4 4.4 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)Nc3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
44301462 18034 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1179075 18034 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL58758 18034 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
90666042 116102 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 550 8 0 9 4.4 Cc1ncccc1-c1nc2cn(-c3cccc(OC(F)F)c3)nc2c(=O)n1C[C@H]1CCCN(C[C@H]2CCCO2)C1 10.1039/C2MD20340E
CHEMBL3218915 116102 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 550 8 0 9 4.4 Cc1ncccc1-c1nc2cn(-c3cccc(OC(F)F)c3)nc2c(=O)n1C[C@H]1CCCN(C[C@H]2CCCO2)C1 10.1039/C2MD20340E
25262771 120241 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 480 7 3 7 3.7 CC(C)NCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319280 120241 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 480 7 3 7 3.7 CC(C)NCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
42624370 195616 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1797 64 25 24 -7.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
44582537 195616 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1797 64 25 24 -7.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
91935104 195616 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1797 64 25 24 -7.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
CHEMBL506624 195616 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1797 64 25 24 -7.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
44445617 161455 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 556 11 2 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccncc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL399649 161455 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 556 11 2 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccncc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
11163070 72342 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 322 5 1 2 4.3 CCN(CC)c1ccc(NC(=O)C2CCc3ccccc3C2)cc1 10.1021/jm0491750
CHEMBL183123 72342 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 322 5 1 2 4.3 CCN(CC)c1ccc(NC(=O)C2CCc3ccccc3C2)cc1 10.1021/jm0491750
156012428 184089 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@H](C)C1 10.1016/j.bmcl.2020.126953
CHEMBL4636832 184089 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@H](C)C1 10.1016/j.bmcl.2020.126953
46882766 12444 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 418 11 4 4 3.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCN)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1077839 12444 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 418 11 4 4 3.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCN)cc2)cc1 10.1016/j.bmcl.2009.08.076
44436813 154085 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 11 4 5 4.5 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](C)N)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL392902 154085 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 11 4 5 4.5 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](C)N)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44410013 83828 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 10 3 7 4.5 CCCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL207268 83828 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 10 3 7 4.5 CCCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44235473 88392 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163478 88392 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
44235473 88392 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163478 88392 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44409839 83033 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 412 7 4 8 2.0 CNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205847 83033 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 412 7 4 8 2.0 CNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
16114099 144002 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 559 10 4 5 5.5 Cc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL375103 144002 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 559 10 4 5 5.5 Cc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
16113372 85929 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCN2)cc1 10.1021/jm0704550
CHEMBL2113319 85929 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCN2)cc1 10.1021/jm0704550
46882273 12590 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 494 10 4 4 5.8 CCCCc1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078982 12590 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 494 10 4 4 5.8 CCCCc1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
122182044 128777 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 552 9 2 6 4.9 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593633 128777 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 552 9 2 6 4.9 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
121879 9015 24 None - 1 Human 5.6 pIC50 = 5.6 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
5868 9015 24 None - 1 Human 5.6 pIC50 = 5.6 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
CHEMBL308716 9015 24 None - 1 Human 5.6 pIC50 = 5.6 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
CHEMBL2370788 216700 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL None None None Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm020985q
145950261 169508 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4171137 169508 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
44394974 73786 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 515 9 1 5 7.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCOCC2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL186974 73786 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 515 9 1 5 7.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCOCC2)cc1 10.1016/j.bmcl.2004.06.060
44445615 168648 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 556 11 2 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2cccnc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL414929 168648 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 556 11 2 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2cccnc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
16113370 85934 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCCN2)cc1 10.1021/jm0704550
CHEMBL2113323 85934 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCCN2)cc1 10.1021/jm0704550
145953016 169366 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
CHEMBL4168863 169366 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
156012445 184114 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637284 184114 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
10186158 105218 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
CHEMBL275660 105218 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
11617435 82772 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 359 5 3 6 4.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2csc(Cl)c2)cc1 10.1021/jm0510934
CHEMBL205486 82772 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 359 5 3 6 4.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2csc(Cl)c2)cc1 10.1021/jm0510934
70696689 82657 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 460 5 0 7 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5cccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048821 82657 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 460 5 0 7 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5cccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
70694647 82643 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 380 6 0 4 3.2 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccccc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048808 82643 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 380 6 0 4 3.2 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccccc2)C3)cc1 10.1016/j.bmcl.2012.05.024
56942242 131973 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 nan
CHEMBL3645257 131973 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 nan
122178605 128119 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581038 128119 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2014.11.031
44445611 161454 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 556 11 2 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL399648 161454 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 556 11 2 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
122182189 128786 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593814 128786 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
56942385 131976 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 nan
CHEMBL3645260 131976 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 nan
CHEMBL501261 220914 23 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)CCCNC(=N)N)C(N)=O 10.1074/jbc.m609796200
56942099 131972 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 nan
CHEMBL3645256 131972 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 nan
56942243 131974 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 nan
CHEMBL3645258 131974 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 nan
122178608 128123 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 570 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(C)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581041 128123 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 570 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(C)n2)cc1 10.1016/j.bmcl.2014.11.031
44409673 83525 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 493 9 3 9 3.9 Cc1ccc(COCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)o1 10.1016/j.bmcl.2006.01.012
CHEMBL206741 83525 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 493 9 3 9 3.9 Cc1ccc(COCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)o1 10.1016/j.bmcl.2006.01.012
CHEMBL105462 215247 38 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
11690097 83447 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 411 6 2 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(N(C)Cc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
CHEMBL206446 83447 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 411 6 2 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(N(C)Cc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
57422695 120253 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 574 10 2 9 4.6 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(-n4cccn4)ccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319401 120253 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 574 10 2 9 4.6 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(-n4cccn4)ccc3Cl)sc2c1 10.1021/jm500610n
25124566 8655 8 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 10.1021/jm5003183
5870 8655 8 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 10.1021/jm5003183
CHEMBL3358452 8655 8 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 10.1021/jm5003183
156013219 184268 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639379 184268 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145957574 169080 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164328 169080 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
46882805 12596 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 474 13 4 4 5.1 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NCC)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079046 12596 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 474 13 4 4 5.1 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NCC)cc2)cc1 10.1016/j.bmcl.2009.08.076
53390538 99052 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 474 5 0 6 4.4 COc1ccc(CC(=O)N2CCC3(CC2)CN(C2CCc4cc(-c5nccs5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426681 99052 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 474 5 0 6 4.4 COc1ccc(CC(=O)N2CCC3(CC2)CN(C2CCc4cc(-c5nccs5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
178024 8752 33 None - 1 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(99)00584-3
5867 8752 33 None - 1 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(99)00584-3
CHEMBL13817 8752 33 None - 1 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(99)00584-3
44445629 168679 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 559 10 2 8 4.9 COc1ccc(-n2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL415136 168679 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 559 10 2 8 4.9 COc1ccc(-n2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
16204239 143062 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
CHEMBL373393 143062 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
11508639 83310 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(Cl)cc2)cc1 10.1021/jm0510934
CHEMBL206091 83310 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(Cl)cc2)cc1 10.1021/jm0510934
216208 16499 33 None - 1 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1016/s0960-894x(99)00584-3
CHEMBL113313 16499 33 None - 1 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1016/s0960-894x(99)00584-3
11846630 145713 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 426 7 3 7 3.7 Nc1nc(N)c(-c2ccc(NC(=O)c3ccncc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL378438 145713 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 426 7 3 7 3.7 Nc1nc(N)c(-c2ccc(NC(=O)c3ccncc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
156012445 184114 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637284 184114 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145953016 169366 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
CHEMBL4168863 169366 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
145949755 169713 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174302 169713 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
16204241 91203 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 520 11 3 5 4.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1CCc1ccccc1 10.1021/jm070024h
CHEMBL221996 91203 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 520 11 3 5 4.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1CCc1ccccc1 10.1021/jm070024h
11221946 147624 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm0510934
CHEMBL381942 147624 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm0510934
11221946 147624 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm060461g
CHEMBL381942 147624 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm060461g
46882104 12727 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 460 12 4 4 4.9 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079873 12727 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 460 12 4 4 4.9 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
145956415 168842 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160541 168842 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145950261 169508 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4171137 169508 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
11654867 82976 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 429 7 3 5 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(CCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205833 82976 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 429 7 3 5 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(CCc2ccccc2)n1 10.1021/jm0510934
10415364 133545 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL365294 133545 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
178024 8752 33 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020985q
5867 8752 33 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020985q
CHEMBL13817 8752 33 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020985q
16114404 161676 24 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 508 11 3 6 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL400814 161676 24 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 508 11 3 6 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1016/j.bmcl.2014.11.031
90666014 116074 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 466 5 0 7 4.6 Cc1ccccc1-c1nc2cn(-c3cccc(C#N)c3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218887 116074 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 466 5 0 7 4.6 Cc1ccccc1-c1nc2cn(-c3cccc(C#N)c3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
44436885 153207 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 634 12 6 8 3.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2c[nH]c3ccccc23)c(OC)c1 10.1021/jm0704550
CHEMBL392191 153207 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 634 12 6 8 3.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2c[nH]c3ccccc23)c(OC)c1 10.1021/jm0704550
44436829 159257 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 11 4 6 4.3 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL397109 159257 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 11 4 6 4.3 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
16114404 161676 24 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 508 11 3 6 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/jm0704550
CHEMBL400814 161676 24 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 508 11 3 6 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/jm0704550
122182047 128780 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA methodAntagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA method
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593636 128780 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA methodAntagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA method
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
70684155 82660 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 486 5 0 6 4.1 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-c3ncccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
CHEMBL2048824 82660 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 486 5 0 6 4.1 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-c3ncccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
CHEMBL2163483 216104 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163483 216104 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44409872 81841 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 467 7 2 8 3.1 CCc1nc(N)nc(N2CCOCC2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203581 81841 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 467 7 2 8 3.1 CCc1nc(N)nc(N2CCOCC2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44445596 161422 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 558 10 2 7 5.5 COc1ccc(-n2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL399448 161422 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 558 10 2 7 5.5 COc1ccc(-n2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
16113692 144014 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 559 11 4 5 5.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
CHEMBL375162 144014 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 559 11 4 5 5.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
118709504 120256 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 572 5 2 9 4.3 Cc1ccnn1-c1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
CHEMBL3319404 120256 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 572 5 2 9 4.3 Cc1ccnn1-c1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
10907396 105926 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 515 10 7 5 1.2 NC1(C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2c[nH]c3ccccc23)NC=O)CCNCC1 10.1021/jm020985q
CHEMBL281147 105926 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 515 10 7 5 1.2 NC1(C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2c[nH]c3ccccc23)NC=O)CCNCC1 10.1021/jm020985q
11677781 131836 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 502 9 1 5 5.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN(C)C(C)=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL364430 131836 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 502 9 1 5 5.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN(C)C(C)=O)cc1 10.1016/j.bmcl.2004.06.060
44445606 161793 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 625 12 3 7 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL401467 161793 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 625 12 3 7 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
44379034 19696 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 490 9 2 5 5.1 NCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1189120 19696 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 490 9 2 5 5.1 NCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL538068 19696 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 490 9 2 5 5.1 NCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
44378986 19867 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 470 10 2 5 3.2 NCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1190325 19867 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 470 10 2 5 3.2 NCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL540603 19867 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 470 10 2 5 3.2 NCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
11697618 69373 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 427 6 1 4 5.5 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Br)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178289 69373 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 427 6 1 4 5.5 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Br)noc2C)cc1 10.1016/j.bmcl.2004.11.075
145956415 168842 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160541 168842 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
44436886 168734 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 595 12 5 8 3.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL415674 168734 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 595 12 5 8 3.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
145949755 169713 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174302 169713 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
23648242 85931 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 571 10 4 5 5.7 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1021/jm0704550
CHEMBL2113320 85931 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 571 10 4 5 5.7 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1021/jm0704550
11606121 71350 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 523 6 2 6 5.9 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.11.075
CHEMBL181584 71350 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 523 6 2 6 5.9 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.11.075
122180023 128362 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 530 7 2 8 3.8 C[C@H]1CN(c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)C[C@@H](C)O1 10.1016/j.bmcl.2015.04.040
CHEMBL3586029 128362 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 530 7 2 8 3.8 C[C@H]1CN(c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)C[C@@H](C)O1 10.1016/j.bmcl.2015.04.040
44379301 19832 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 506 9 2 7 3.7 COC(=O)C(CCCCN)NC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Cl)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1190091 19832 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 506 9 2 7 3.7 COC(=O)C(CCCCN)NC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Cl)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL540093 19832 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 506 9 2 7 3.7 COC(=O)C(CCCCN)NC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Cl)cc2c1=O 10.1016/s0960-894x(99)00584-3
44338300 174622 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 525 10 1 6 4.0 CN(C)CCCN1C(=O)[C@H](Cc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=S 10.1016/j.bmcl.2003.11.012
CHEMBL430882 174622 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 525 10 1 6 4.0 CN(C)CCCN1C(=O)[C@H](Cc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=S 10.1016/j.bmcl.2003.11.012
44338239 174677 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 511 9 1 6 4.2 CN(C)CCCN1C(=O)[C@H](c2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=S 10.1016/j.bmcl.2003.11.012
CHEMBL431245 174677 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 511 9 1 6 4.2 CN(C)CCCN1C(=O)[C@H](c2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=S 10.1016/j.bmcl.2003.11.012
44409762 82661 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 441 9 4 8 2.7 CCc1nc(N)nc(NCCO)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204884 82661 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 441 9 4 8 2.7 CCc1nc(N)nc(NCCO)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122180018 128357 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 527 9 2 9 4.3 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586024 128357 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 527 9 2 9 4.3 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
122182189 128786 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Antagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA methodAntagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA method
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593814 128786 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Antagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA methodAntagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA method
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
10032659 18823 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 587 11 4 8 -0.5 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@H](CO)NC(=O)CN)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL1183505 18823 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 587 11 4 8 -0.5 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@H](CO)NC(=O)CN)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL301259 18823 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 587 11 4 8 -0.5 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@H](CO)NC(=O)CN)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
60195019 88379 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 849 21 10 8 2.2 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163464 88379 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 849 21 10 8 2.2 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
156009875 183902 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633695 183902 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
11430583 86992 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 439 8 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL213704 86992 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 439 8 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
11517629 175117 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 431 6 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C)c1 10.1016/j.bmcl.2004.11.075
CHEMBL434330 175117 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 431 6 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C)c1 10.1016/j.bmcl.2004.11.075
44409975 82565 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 411 7 3 7 3.3 CCc1nc(N)nc(NC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204835 82565 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 411 7 3 7 3.3 CCc1nc(N)nc(NC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
53391301 99049 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN(C2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426678 99049 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN(C2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
90666019 116079 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 464 7 0 8 3.8 COCCN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(C4CCCCC4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218892 116079 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 464 7 0 8 3.8 COCCN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(C4CCCCC4)nc3c2=O)C1 10.1039/C2MD20340E
11669486 71388 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 445 7 1 4 6.6 CCc1cc(N(CC)CC)ccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
CHEMBL181736 71388 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 445 7 1 4 6.6 CCc1cc(N(CC)CC)ccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
59446141 88395 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(CCc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163481 88395 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(CCc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
59446141 88395 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(CCc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163481 88395 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(CCc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44436917 97424 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 4 5 5.3 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL239007 97424 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 4 5 5.3 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
60165265 122976 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 453 5 1 2 6.0 CC(NC(=O)N(Cc1ccccc1Cl)C1CCN(C)CC1)c1cccc(Cl)c1Cl 10.1021/jm5003183
CHEMBL3358453 122976 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 453 5 1 2 6.0 CC(NC(=O)N(Cc1ccccc1Cl)C1CCN(C)CC1)c1cccc(Cl)c1Cl 10.1021/jm5003183
16113002 155092 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 577 12 4 7 4.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)c(OC)c1 10.1021/jm0704550
CHEMBL393693 155092 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 577 12 4 7 4.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)c(OC)c1 10.1021/jm0704550
44409678 147995 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 490 9 3 9 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3cccnc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL382853 147995 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 490 9 3 9 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3cccnc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
122178604 128118 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2N)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581037 128118 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2N)cc1 10.1016/j.bmcl.2014.11.031
10929048 75582 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 488 9 6 4 2.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL19220 75582 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 488 9 6 4 2.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
60195018 88378 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 834 21 9 7 3.2 CCC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NN(CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163463 88378 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 834 21 9 7 3.2 CCC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NN(CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44394913 133951 1 None - 0 Human 6.4 pIC50 = 6.4 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 537 10 1 5 7.5 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccccc2OC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL365721 133951 1 None - 0 Human 6.4 pIC50 = 6.4 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 537 10 1 5 7.5 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccccc2OC)cc1 10.1016/j.bmcl.2004.06.060
11649248 73444 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 515 9 1 5 7.2 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL185399 73444 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 515 9 1 5 7.2 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCCO2)cc1 10.1016/j.bmcl.2004.06.060
44394833 133603 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 542 9 1 5 6.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2C(=O)CCC2(C)C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL365460 133603 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 542 9 1 5 6.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2C(=O)CCC2(C)C)cc1 10.1016/j.bmcl.2004.06.060
11827047 105996 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 488 11 6 4 2.1 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC=O 10.1021/jm020985q
CHEMBL281578 105996 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 488 11 6 4 2.1 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC=O 10.1021/jm020985q
42624359 200180 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1755 61 25 24 -8.1 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
44582536 200180 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1755 61 25 24 -8.1 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
91935103 200180 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1755 61 25 24 -8.1 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
CHEMBL525751 200180 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1755 61 25 24 -8.1 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
156009875 183902 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633695 183902 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156021942 185002 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4649860 185002 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
122180021 128360 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 528 7 2 7 4.9 O=C(NCC1COc2ccccc2O1)c1cc(-c2ccnc(Cl)c2)cnc1NCc1ccc2c(c1)OCC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586027 128360 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 528 7 2 7 4.9 O=C(NCC1COc2ccccc2O1)c1cc(-c2ccnc(Cl)c2)cnc1NCc1ccc2c(c1)OCC2 10.1016/j.bmcl.2015.04.040
11134880 106207 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 500 10 6 4 2.1 O=CN[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCNCC1 10.1021/jm020985q
CHEMBL282891 106207 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 500 10 6 4 2.1 O=CN[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCNCC1 10.1021/jm020985q
11846629 145597 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 419 7 3 7 3.1 Nc1nc(N)c(-c2ccc(NC(=O)C3CCCO3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL378118 145597 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 419 7 3 7 3.1 Nc1nc(N)c(-c2ccc(NC(=O)C3CCCO3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
11114279 105025 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 544 12 6 4 3.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(C)C 10.1021/jm020985q
CHEMBL274460 105025 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 544 12 6 4 3.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(C)C 10.1021/jm020985q
145952396 169782 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
CHEMBL4175534 169782 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
122178607 128122 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 592 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncc(F)cc2F)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581040 128122 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 592 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncc(F)cc2F)cc1 10.1016/j.bmcl.2014.11.031
156013219 184268 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639379 184268 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145957574 169080 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164328 169080 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
11846463 146020 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 422 5 2 8 2.7 CCc1nc(N)nc(N)c1-c1ccc2c(c1)ncn2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
CHEMBL378909 146020 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 422 5 2 8 2.7 CCc1nc(N)nc(N)c1-c1ccc2c(c1)ncn2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
9890863 138770 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CC)CCN1C(=O)C(O)(c2ccccc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL369533 138770 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CC)CCN1C(=O)C(O)(c2ccccc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
44409864 82274 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 502 9 3 8 4.0 CN(Cc1ccccc1)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204266 82274 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 502 9 3 8 4.0 CN(Cc1ccccc1)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122180027 128366 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 566 8 2 7 5.2 CC(C)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586033 128366 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 566 8 2 7 5.2 CC(C)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
11430392 83499 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 431 6 3 7 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Cl)c1 10.1021/jm0510934
CHEMBL206588 83499 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 431 6 3 7 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Cl)c1 10.1021/jm0510934
57785737 120219 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 549 7 2 8 3.7 CN1CCCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319216 120219 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 549 7 2 8 3.7 CN1CCCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
44390871 71616 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2c(Cl)cccc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL182035 71616 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2c(Cl)cccc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
70682037 82656 20 None 43 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 495 5 0 8 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048820 82656 20 None 43 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 495 5 0 8 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1 10.1016/j.bmcl.2012.05.024
156021297 184868 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647797 184868 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
90666040 116100 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 542 9 0 9 4.6 CCCOc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218913 116100 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 542 9 0 9 4.6 CCCOc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
90666026 116086 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 516 9 0 9 4.1 CCO[C@H](C)CN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218899 116086 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 516 9 0 9 4.1 CCO[C@H](C)CN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
16204021 91482 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 10 3 5 4.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(F)cc1 10.1021/jm070024h
CHEMBL222710 91482 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 10 3 5 4.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(F)cc1 10.1021/jm070024h
122180014 128353 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 539 9 2 8 5.8 CCCn1cc(-c2cnc(NCc3ccc4sccc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586020 128353 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 539 9 2 8 5.8 CCCn1cc(-c2cnc(NCc3ccc4sccc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
90666016 116076 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 481 5 0 9 2.9 Cc1ncccc1-c1nc2cn(-c3ccc(C#N)cc3)nc2c(=O)n1CC1CCCN(C2COC2)C1 10.1039/C2MD20340E
CHEMBL3218889 116076 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 481 5 0 9 2.9 Cc1ncccc1-c1nc2cn(-c3ccc(C#N)cc3)nc2c(=O)n1CC1CCCN(C2COC2)C1 10.1039/C2MD20340E
44389186 71389 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 379 7 1 5 4.8 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3OC)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL181739 71389 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 379 7 1 5 4.8 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3OC)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44338266 117110 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 523 11 1 6 4.3 CN(C)CCCN1C(=O)[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=O 10.1016/j.bmcl.2003.11.012
CHEMBL323974 117110 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 523 11 1 6 4.3 CN(C)CCCN1C(=O)[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=O 10.1016/j.bmcl.2003.11.012
70692602 82651 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 423 8 0 5 3.5 CCCOc1ccc(CN2CC3(CCN(C(=O)Cc4ccc(OC)cc4)CC3)C2)cn1 10.1016/j.bmcl.2012.05.024
CHEMBL2048815 82651 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 423 8 0 5 3.5 CCCOc1ccc(CN2CC3(CCN(C(=O)Cc4ccc(OC)cc4)CC3)C2)cn1 10.1016/j.bmcl.2012.05.024
11455251 168093 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 523 8 3 7 5.0 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3Br)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL412362 168093 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 523 8 3 7 5.0 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3Br)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
156021942 185002 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4649860 185002 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
16204037 144011 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccccc1Cn1c(Cc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL375150 144011 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccccc1Cn1c(Cc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
11582836 69687 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 431 7 1 4 6.4 CCCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178463 69687 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 431 7 1 4 6.4 CCCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44389131 70236 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 485 6 1 4 7.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C(F)(F)F)c1 10.1016/j.bmcl.2004.11.075
CHEMBL179812 70236 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 485 6 1 4 7.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C(F)(F)F)c1 10.1016/j.bmcl.2004.11.075
122180025 128364 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 542 7 2 8 3.6 CC(=O)N1CC=C(c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)CC1 10.1016/j.bmcl.2015.04.040
CHEMBL3586031 128364 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 542 7 2 8 3.6 CC(=O)N1CC=C(c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)CC1 10.1016/j.bmcl.2015.04.040
122178612 128127 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 572 11 2 6 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc[n+]2[O-])cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581045 128127 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 572 11 2 6 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc[n+]2[O-])cc1 10.1016/j.bmcl.2014.11.031
16203237 103726 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 496 10 3 6 4.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccco1 10.1021/jm070024h
CHEMBL266199 103726 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 496 10 3 6 4.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccco1 10.1021/jm070024h
59446148 181828 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 840 21 10 9 1.3 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(CC1CCCCC1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4567800 181828 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 840 21 10 9 1.3 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(CC1CCCCC1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
46882152 12627 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 432 12 4 4 4.1 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(CCCN)c2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079302 12627 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 432 12 4 4 4.1 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(CCCN)c2)cc1 10.1016/j.bmcl.2009.08.076
11655355 81196 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)s3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL202642 81196 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)s3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
145952396 169782 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
CHEMBL4175534 169782 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
46882764 12403 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 375 9 3 3 4.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1077716 12403 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 375 9 3 3 4.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1016/j.bmcl.2009.08.076
16114290 143986 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 534 11 3 5 5.3 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL374992 143986 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 534 11 3 5 5.3 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
90666015 116075 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 483 7 0 9 3.2 COCCN1CCCC(Cn2c(-c3cccnc3C)nc3cn(-c4ccc(C#N)cc4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218888 116075 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 483 7 0 9 3.2 COCCN1CCCC(Cn2c(-c3cccnc3C)nc3cn(-c4ccc(C#N)cc4)nc3c2=O)C1 10.1039/C2MD20340E
44436831 158775 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 580 12 4 7 4.3 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL396681 158775 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 580 12 4 7 4.3 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
25262608 120240 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 492 6 2 7 3.8 O=C(NC(=O)c1ccccc1Cl)Nc1nc2ccc(S(=O)(=O)CCN3CCCC3)cc2s1 10.1021/jm500610n
CHEMBL3319279 120240 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 492 6 2 7 3.8 O=C(NC(=O)c1ccccc1Cl)Nc1nc2ccc(S(=O)(=O)CCN3CCCC3)cc2s1 10.1021/jm500610n
10918326 105748 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N(C)C 10.1021/jm020985q
CHEMBL279822 105748 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N(C)C 10.1021/jm020985q
16203918 91562 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 570 9 3 5 5.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1ccc(Br)cc1 10.1021/jm070024h
CHEMBL223239 91562 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 570 9 3 5 5.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1ccc(Br)cc1 10.1021/jm070024h
70696687 82648 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 446 7 0 6 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4cccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048812 82648 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 446 7 0 6 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4cccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
46882105 13123 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 460 12 4 4 4.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)CN)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1082044 13123 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 460 12 4 4 4.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)CN)cc2)cc1 10.1016/j.bmcl.2009.08.076
44446189 162153 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL403426 162153 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
44446157 101427 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 594 13 3 8 4.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](CC(=O)OCc2ccccc2)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252501 101427 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 594 13 3 8 4.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](CC(=O)OCc2ccccc2)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
44446148 162197 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL403683 162197 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
44410008 148029 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 9 2 7 4.2 CCc1nc(N)nc(N(CC)CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL383058 148029 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 9 2 7 4.2 CCc1nc(N)nc(N(CC)CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
59446143 88375 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 802 17 11 8 0.6 C[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O nan
CHEMBL2163448 88375 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 802 17 11 8 0.6 C[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O nan
59446143 88375 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 802 17 11 8 0.6 C[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1021/jm300557t
CHEMBL2163448 88375 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 802 17 11 8 0.6 C[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1021/jm300557t
44338221 14820 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 581 11 1 7 4.2 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=S)N1CCCN1CCOCC1 10.1016/j.bmcl.2003.11.012
CHEMBL109094 14820 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 581 11 1 7 4.2 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=S)N1CCCN1CCOCC1 10.1016/j.bmcl.2003.11.012
60195113 88382 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 787 17 9 7 2.5 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm300557t
CHEMBL2163467 88382 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 787 17 9 7 2.5 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm300557t
46882804 12595 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 446 11 4 4 4.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079045 12595 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 446 11 4 4 4.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
10864048 105164 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.6 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL275373 105164 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.6 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
156016110 184477 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 628 7 1 9 5.1 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccc(S(=O)(=O)C5CCN(C)CC5)cc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4642043 184477 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 628 7 1 9 5.1 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccc(S(=O)(=O)C5CCN(C)CC5)cc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
156017268 184429 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641472 184429 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
59446118 181479 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)N(Cc1cccc2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4559602 181479 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)N(Cc1cccc2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
60195285 88387 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)N(Cc1cccc2ccccc12)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163473 88387 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)N(Cc1cccc2ccccc12)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44436868 152861 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 520 9 4 5 4.6 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1c1ccccc1)C1CCNCC1 10.1021/jm0704550
CHEMBL391922 152861 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 520 9 4 5 4.6 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1c1ccccc1)C1CCNCC1 10.1021/jm0704550
44394947 176002 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL440939 176002 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)cc1 10.1016/j.bmcl.2004.06.060
122180022 128361 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 504 7 2 9 2.8 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2CCOCC2)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
CHEMBL3586028 128361 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 504 7 2 9 2.8 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2CCOCC2)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
11751384 148284 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 453 9 3 6 4.6 Nc1nc(N)c(-c2ccc(NC(=O)CCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL384524 148284 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 453 9 3 6 4.6 Nc1nc(N)c(-c2ccc(NC(=O)CCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
122180026 128365 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 566 7 2 7 4.4 CC(=O)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586032 128365 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 566 7 2 7 4.4 CC(=O)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
122182043 128776 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 580 7 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593632 128776 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 580 7 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
16204226 91574 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 486 12 3 5 5.1 CCCCCCn1c(Cc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL223323 91574 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 486 12 3 5 5.1 CCCCCCn1c(Cc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
118709472 120239 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 409 3 2 6 3.3 CS(=O)(=O)c1ccc2sc(NC(=O)NC(=O)c3ccccc3Cl)nc2c1 10.1021/jm500610n
CHEMBL3319277 120239 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 409 3 2 6 3.3 CS(=O)(=O)c1ccc2sc(NC(=O)NC(=O)c3ccccc3Cl)nc2c1 10.1021/jm500610n
46882196 12513 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 418 9 4 4 3.7 CCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078402 12513 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 418 9 4 4 3.7 CCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
44379303 19611 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 468 11 2 5 4.1 NCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1188529 19611 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 468 11 2 5 4.1 NCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL536706 19611 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 468 11 2 5 4.1 NCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL2310893 216275 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C(C)C 10.1021/jm0001727
44445614 176088 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 554 11 2 5 6.0 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2cccnc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL441567 176088 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 554 11 2 5 6.0 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2cccnc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
44445598 101151 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 565 9 3 5 6.5 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL250807 101151 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 565 9 3 5 6.5 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
145949381 169494 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4170865 169494 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
44436832 158777 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 548 11 4 5 4.9 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL396682 158777 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 548 11 4 5 4.9 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44445626 103841 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 573 11 2 8 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL267197 103841 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 573 11 2 8 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
90666025 116085 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 516 9 0 9 4.1 CCO[C@@H](C)CN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218898 116085 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 516 9 0 9 4.1 CCO[C@@H](C)CN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
156012122 184160 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637980 184160 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156012122 184160 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637980 184160 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156021297 184868 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647797 184868 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
90666024 116084 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218897 116084 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
57422776 120221 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 559 7 2 8 3.3 C#Cc1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
CHEMBL3319218 120221 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 559 7 2 8 3.3 C#Cc1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
162657463 187819 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting methodDisplacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting method
ChEMBL 783 20 7 7 4.0 NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)C(N)=O 10.1016/j.ejmech.2016.07.078
CHEMBL4759415 187819 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting methodDisplacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting method
ChEMBL 783 20 7 7 4.0 NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)C(N)=O 10.1016/j.ejmech.2016.07.078
44409990 83292 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 481 12 3 7 5.2 CCCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205995 83292 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 481 12 3 7 5.2 CCCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122180024 128363 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 530 7 2 9 3.4 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2C[C@@H]3CC[C@H](C2)O3)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
CHEMBL3586030 128363 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 530 7 2 9 3.4 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2C[C@@H]3CC[C@H](C2)O3)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
44409758 82749 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 411 6 3 7 3.4 CC(C)c1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205374 82749 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 411 6 3 7 3.4 CC(C)c1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122182190 128787 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
CHEMBL3593815 128787 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
44409684 147663 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 474 8 4 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL382033 147663 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 474 8 4 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
16113003 101522 2 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 617 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)c(OC)c1 10.1021/jm701292s
CHEMBL253126 101522 2 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 617 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)c(OC)c1 10.1021/jm701292s
16113003 101522 2 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 617 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)c(OC)c1 10.1021/jm0704550
CHEMBL253126 101522 2 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 617 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)c(OC)c1 10.1021/jm0704550
122182047 128780 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593636 128780 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
90666030 116090 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 486 7 0 8 4.3 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218903 116090 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 486 7 0 8 4.3 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
11605333 83500 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 475 6 3 7 3.6 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Br)c1 10.1021/jm0510934
CHEMBL206589 83500 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 475 6 3 7 3.6 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Br)c1 10.1021/jm0510934
122182046 128779 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 586 8 2 6 5.6 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCC3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593635 128779 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 586 8 2 6 5.6 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCC3)cc1Cl 10.1016/j.bmc.2015.05.047
11281346 82793 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 411 8 3 6 4.6 Nc1nc(N)c(-c2ccc(NCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205568 82793 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 411 8 3 6 4.6 Nc1nc(N)c(-c2ccc(NCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
145949381 169494 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4170865 169494 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
16204145 143330 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 492 9 3 5 4.5 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1ccccc1 10.1021/jm070024h
CHEMBL373772 143330 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 492 9 3 5 4.5 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1ccccc1 10.1021/jm070024h
90666036 116096 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 479 8 0 8 3.7 COc1cccc(-n2cc3nc(CC(C)C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218909 116096 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 479 8 0 8 3.7 COc1cccc(-n2cc3nc(CC(C)C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
44338235 116439 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 546 7 3 6 4.1 O=C1[C@H](Cc2c[nH]c3ccccc23)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=O)N1C1CCNCC1 10.1016/j.bmcl.2003.11.012
CHEMBL322499 116439 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 546 7 3 6 4.1 O=C1[C@H](Cc2c[nH]c3ccccc23)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=O)N1C1CCNCC1 10.1016/j.bmcl.2003.11.012
156016392 184425 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641386 184425 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156017268 184429 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641472 184429 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145958317 169092 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164531 169092 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145949880 169570 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4172217 169570 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
145950963 169585 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4172411 169585 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
156016392 184425 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641386 184425 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44445608 161794 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 554 11 2 5 6.0 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL401468 161794 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 554 11 2 5 6.0 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
59446116 88373 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 777 17 9 8 0.8 C[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)N(Cc1ccccc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1021/jm300557t
CHEMBL2163439 88373 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 777 17 9 8 0.8 C[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)N(Cc1ccccc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1021/jm300557t
23631387 100041 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 409 4 0 4 5.1 Cc1nc2ccc(-c3ccc(Cl)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL244936 100041 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 409 4 0 4 5.1 Cc1nc2ccc(-c3ccc(Cl)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1039/C2MD20340E
90666038 116098 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1ccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)cc1 10.1039/C2MD20340E
CHEMBL3218911 116098 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1ccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)cc1 10.1039/C2MD20340E
44421230 91566 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 546 8 3 5 5.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1-c1ccc(Cl)c(Cl)c1 10.1021/jm070024h
CHEMBL223269 91566 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 546 8 3 5 5.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1-c1ccc(Cl)c(Cl)c1 10.1021/jm070024h
156018460 184656 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 468 5 1 7 4.6 CCOc1cc(Cl)c(-c2ncc(-c3nc4ccccc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4644587 184656 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 468 5 1 7 4.6 CCOc1cc(Cl)c(-c2ncc(-c3nc4ccccc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
145950963 169585 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4172411 169585 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
11618705 173717 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 423 6 1 4 5.3 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL428698 173717 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 423 6 1 4 5.3 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)CC1 10.1016/j.bmcl.2004.06.060
44436842 153716 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCCCN2)cc1 10.1021/jm0704550
CHEMBL392592 153716 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCCCN2)cc1 10.1021/jm0704550
CHEMBL509976 222359 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
CHEMBL450217 220742 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in COS-7 cells incubated for 3 hrsDisplacement of [35S]MK677 from human ghrelin receptor expressed in COS-7 cells incubated for 3 hrs
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm300414b
CHEMBL450217 220742 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1c[nH]c2ccccc12)C(N)=O 10.1074/jbc.m609796200
10984270 105283 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 530 11 6 4 3.3 CC(C)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL276137 105283 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 530 11 6 4 3.3 CC(C)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
44436884 98327 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 565 11 5 7 3.1 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL240522 98327 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 565 11 5 7 3.1 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL444131 220708 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None NC(=O)CNC(=O)CNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1c[nH]c2ccccc12 10.1074/jbc.m609796200
60195020 88380 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 835 21 10 8 1.8 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163465 88380 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 835 21 10 8 1.8 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
59446112 179753 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 840 21 10 9 1.3 C[C@H](NC(=O)N(CC1CCCCC1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4517723 179753 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 840 21 10 9 1.3 C[C@H](NC(=O)N(CC1CCCCC1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL422461 220065 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm0001727
16114010 143061 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 613 10 4 5 6.5 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(Cl)c(Cl)c1 10.1021/jm070024h
CHEMBL373392 143061 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 613 10 4 5 6.5 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(Cl)c(Cl)c1 10.1021/jm070024h
16203349 173069 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 12 3 6 4.9 COc1ccc(CCn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL427076 173069 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 12 3 6 4.9 COc1ccc(CCn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
11531313 69278 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 394 7 1 6 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3[N+](=O)[O-])noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178137 69278 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 394 7 1 6 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3[N+](=O)[O-])noc2C)cc1 10.1016/j.bmcl.2004.11.075
44389283 69719 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 403 5 1 4 5.7 CCN(C)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178494 69719 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 403 5 1 4 5.7 CCN(C)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
122180019 128358 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586025 128358 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL447282 220728 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
ChEMBL None None None CCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm8014519
145958317 169092 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164531 169092 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
16114008 91621 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccccc1Cn1c(CCc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL223532 91621 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccccc1Cn1c(CCc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
16112910 143155 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 552 11 3 7 4.6 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
CHEMBL373507 143155 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 552 11 3 7 4.6 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
16112910 143155 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 552 11 3 7 4.6 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL373507 143155 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 552 11 3 7 4.6 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
44436882 152794 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 10 4 6 4.2 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1Cc1ccco1)C1CCNCC1 10.1021/jm0704550
CHEMBL391859 152794 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 10 4 6 4.2 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1Cc1ccco1)C1CCNCC1 10.1021/jm0704550
145949880 169570 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4172217 169570 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
122180024 128363 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 530 7 2 9 3.4 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2C[C@@H]3CC[C@H](C2)O3)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
CHEMBL3586030 128363 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 530 7 2 9 3.4 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2C[C@@H]3CC[C@H](C2)O3)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
46882154 12633 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 390 7 4 4 2.9 CCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079323 12633 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 390 7 4 4 2.9 CCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
59446145 88374 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 793 19 11 8 0.8 C[C@H](N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163444 88374 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 793 19 11 8 0.8 C[C@H](N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
59446145 88374 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 793 19 11 8 0.8 C[C@H](N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163444 88374 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 793 19 11 8 0.8 C[C@H](N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
11699004 72977 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 501 9 1 5 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL184429 72977 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 501 9 1 5 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)cc1 10.1016/j.bmcl.2004.06.060
11537800 82342 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 361 6 3 6 3.7 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)=O)cc2)cc1 10.1021/jm0510934
CHEMBL204564 82342 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 361 6 3 6 3.7 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)=O)cc2)cc1 10.1021/jm0510934
16203236 173041 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 512 10 3 6 4.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1cccs1 10.1021/jm070024h
CHEMBL426905 173041 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 512 10 3 6 4.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1cccs1 10.1021/jm070024h
10207327 73845 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
CHEMBL18725 73845 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
44445603 161759 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 572 11 2 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccncc2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL401259 161759 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 572 11 2 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccncc2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL502208 220929 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1074/jbc.m609796200
16113583 168530 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 469 8 4 5 3.7 Cn1c(CCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL413856 168530 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 469 8 4 5 3.7 Cn1c(CCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
90665849 116053 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 508 7 0 7 5.5 COCCN1CCC[C@@H](Cn2c(-c3ccccc3C)nc3nc(-c4ccc(Cl)cc4)sc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218649 116053 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 508 7 0 7 5.5 COCCN1CCC[C@@H](Cn2c(-c3ccccc3C)nc3nc(-c4ccc(Cl)cc4)sc3c2=O)C1 10.1039/C2MD20340E
70696688 82654 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 487 9 0 6 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cn1 10.1016/j.bmcl.2012.05.024
CHEMBL2048818 82654 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 487 9 0 6 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cn1 10.1016/j.bmcl.2012.05.024
44436816 98580 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 12 4 6 3.9 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CCN)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL241242 98580 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 12 4 6 3.9 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CCN)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
10984270 105283 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 530 11 6 4 3.3 CC(C)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL276137 105283 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 530 11 6 4 3.3 CC(C)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
44301387 18036 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1179088 18036 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL59572 18036 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
11692087 69766 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL178610 69766 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.06.060
122178610 128125 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(N)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581043 128125 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(N)n2)cc1 10.1016/j.bmcl.2014.11.031
16113695 143805 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm701292s
CHEMBL374643 143805 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm701292s
16113695 143805 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL374643 143805 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
16113695 143805 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL374643 143805 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
16113695 143805 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm0704550
CHEMBL374643 143805 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm0704550
44436888 159835 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 565 11 3 6 5.0 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCOCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL397593 159835 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 565 11 3 6 5.0 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCOCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
11692087 69766 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178610 69766 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.11.075
44409809 81840 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 10 3 7 4.4 CCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203578 81840 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 10 3 7 4.4 CCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409989 172605 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 467 11 3 7 4.8 CCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL424860 172605 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 467 11 3 7 4.8 CCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL105462 215247 38 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
90666018 116078 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 488 8 0 9 3.3 COCCN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218891 116078 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 488 8 0 9 3.3 COCCN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
11612155 147787 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3csc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL382375 147787 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3csc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
118722878 122975 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 494 5 2 4 4.8 CN1CCN([C@@H](C(=O)NNc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2Cl)CC1 10.1021/jm5003183
CHEMBL3358451 122975 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 494 5 2 4 4.8 CN1CCN([C@@H](C(=O)NNc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2Cl)CC1 10.1021/jm5003183
16114097 85932 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCCNC2)c(OC)c1 10.1021/jm0704550
CHEMBL2113321 85932 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCCNC2)c(OC)c1 10.1021/jm0704550
122182189 128786 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593814 128786 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
25260901 120257 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 577 5 2 9 3.6 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319405 120257 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 577 5 2 9 3.6 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
122180021 128360 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 528 7 2 7 4.9 O=C(NCC1COc2ccccc2O1)c1cc(-c2ccnc(Cl)c2)cnc1NCc1ccc2c(c1)OCC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586027 128360 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 528 7 2 7 4.9 O=C(NCC1COc2ccccc2O1)c1cc(-c2ccnc(Cl)c2)cnc1NCc1ccc2c(c1)OCC2 10.1016/j.bmcl.2015.04.040
11179347 84128 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 490 9 2 8 4.0 CS(=O)(=O)c1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL208477 84128 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 490 9 2 8 4.0 CS(=O)(=O)c1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
44445593 161566 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 552 11 3 7 4.6 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)C(C)(C)N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL400174 161566 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 552 11 3 7 4.6 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)C(C)(C)N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
16203569 148511 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
CHEMBL385803 148511 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
90666034 116094 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.7 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCOC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218907 116094 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.7 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCOC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL449590 220741 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1074/jbc.m609796200
121879 9015 24 None - 1 Rat 7.2 pIC50 = 7.2 Binding
Inhibition against rat growth hormone secretagogue (GHS) receptorInhibition against rat growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
5868 9015 24 None - 1 Rat 7.2 pIC50 = 7.2 Binding
Inhibition against rat growth hormone secretagogue (GHS) receptorInhibition against rat growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
CHEMBL308716 9015 24 None - 1 Rat 7.2 pIC50 = 7.2 Binding
Inhibition against rat growth hormone secretagogue (GHS) receptorInhibition against rat growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
11568561 176333 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 447 7 1 5 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(OC)c1 10.1016/j.bmcl.2004.11.075
CHEMBL443560 176333 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 447 7 1 5 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(OC)c1 10.1016/j.bmcl.2004.11.075
44338246 105630 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 563 11 1 6 5.2 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
CHEMBL278909 105630 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 563 11 1 6 5.2 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
CHEMBL105462 215247 38 None - 1 Human 5.2 pIC50 = 5.2 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/s0960-894x(99)00584-3
44409767 164021 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 437 8 3 7 3.9 CCc1nc(N)nc(NC2CC2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL407647 164021 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 437 8 3 7 3.9 CCc1nc(N)nc(NC2CC2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44445612 103815 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 565 10 3 5 5.9 O=C(Cc1ccccn1)N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm701292s
CHEMBL266964 103815 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 565 10 3 5 5.9 O=C(Cc1ccccn1)N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm701292s
44410003 82956 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 468 10 4 8 3.5 CC(C)CCNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205794 82956 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 468 10 4 8 3.5 CC(C)CCNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
16203569 148511 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL385803 148511 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL18872 215837 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(C)(C)N)C(N)=O 10.1021/jm300557t
46882106 12634 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 418 11 4 4 3.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(CCN)c2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079340 12634 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 418 11 4 4 3.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(CCN)c2)cc1 10.1016/j.bmcl.2009.08.076
44436876 153797 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 580 11 4 7 4.6 COc1ccc(N2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL392663 153797 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 580 11 4 7 4.6 COc1ccc(N2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
121879 9015 24 None - 1 Pig 7.2 pIC50 = 7.2 Binding
Inhibition against pig growth hormone secretagogue (GHS) receptorInhibition against pig growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
5868 9015 24 None - 1 Pig 7.2 pIC50 = 7.2 Binding
Inhibition against pig growth hormone secretagogue (GHS) receptorInhibition against pig growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
CHEMBL308716 9015 24 None - 1 Pig 7.2 pIC50 = 7.2 Binding
Inhibition against pig growth hormone secretagogue (GHS) receptorInhibition against pig growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
156010733 183859 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633062 183859 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145962494 168853 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160705 168853 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145950201 169721 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174476 169721 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
44409832 83185 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 398 6 4 8 1.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205955 83185 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 398 6 4 8 1.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN)cc2)cc1 10.1016/j.bmcl.2006.01.012
16204237 91672 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 574 10 3 5 6.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(Cl)c(Cl)c1 10.1021/jm070024h
CHEMBL223638 91672 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 574 10 3 5 6.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(Cl)c(Cl)c1 10.1021/jm070024h
16204343 143969 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 635 12 4 5 7.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1CC(c1ccccc1)c1ccccc1 10.1021/jm070024h
CHEMBL374918 143969 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 635 12 4 5 7.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1CC(c1ccccc1)c1ccccc1 10.1021/jm070024h
122178613 128128 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 625 12 2 7 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(N3CCCC3)cn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581046 128128 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 625 12 2 7 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(N3CCCC3)cn2)cc1 10.1016/j.bmcl.2014.11.031
57422749 120216 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 492 4 2 7 3.8 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319213 120216 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 492 4 2 7 3.8 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
44410007 83202 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 438 8 4 8 2.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205963 83202 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 438 8 4 8 2.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
118718706 122157 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL3350011 122157 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
89768546 155796 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of ghrelin receptor (unknown origin) by radioligand binding assayInhibition of ghrelin receptor (unknown origin) by radioligand binding assay
ChEMBL 438 4 2 5 5.5 Cc1nnc2sc(C(=O)NCc3ccc(S(F)(F)(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3942511 155796 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of ghrelin receptor (unknown origin) by radioligand binding assayInhibition of ghrelin receptor (unknown origin) by radioligand binding assay
ChEMBL 438 4 2 5 5.5 Cc1nnc2sc(C(=O)NCc3ccc(S(F)(F)(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
16114011 144916 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 563 10 4 5 5.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(F)cc1 10.1021/jm070024h
CHEMBL376736 144916 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 563 10 4 5 5.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(F)cc1 10.1021/jm070024h
11349789 85548 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 389 7 3 6 3.4 Nc1nc(N)c(-c2ccc(NC(=O)C3CC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL211265 85548 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 389 7 3 6 3.4 Nc1nc(N)c(-c2ccc(NC(=O)C3CC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
16112909 151059 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 561 10 4 6 5.0 COc1ccc(Cn2c(Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL390503 151059 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 561 10 4 6 5.0 COc1ccc(Cn2c(Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
44378837 19793 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 484 11 2 5 3.6 NCCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1189851 19793 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 484 11 2 5 3.6 NCCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL539575 19793 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 484 11 2 5 3.6 NCCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
44445597 101291 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 540 10 2 5 6.1 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL251640 101291 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 540 10 2 5 6.1 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
11176805 84109 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 391 7 3 6 4.5 CC(C)(C)CNc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm0510934
CHEMBL208374 84109 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 391 7 3 6 4.5 CC(C)(C)CNc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm0510934
156010733 183859 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633062 183859 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
46882153 12632 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 528 13 4 4 5.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NCC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079322 12632 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 528 13 4 4 5.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NCC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.08.076
145950201 169721 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174476 169721 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
46882239 12556 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 7 4 4 4.7 Cc1cccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)c1 10.1016/j.bmcl.2009.08.076
CHEMBL1078700 12556 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 7 4 4 4.7 Cc1cccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)c1 10.1016/j.bmcl.2009.08.076
1221269 128812 12 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL359530 128812 12 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44446177 101422 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252448 101422 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
16114289 105441 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCNC2)cc1 10.1021/jm0704550
CHEMBL277376 105441 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCNC2)cc1 10.1021/jm0704550
11538533 81776 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm060461g
CHEMBL203280 81776 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm060461g
10415364 133545 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against mouse Growth hormone secretagogue receptorInhibitory concentration against mouse Growth hormone secretagogue receptor
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL365294 133545 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against mouse Growth hormone secretagogue receptorInhibitory concentration against mouse Growth hormone secretagogue receptor
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL263544 217354 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0001727
122180023 128362 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 530 7 2 8 3.8 C[C@H]1CN(c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)C[C@@H](C)O1 10.1016/j.bmcl.2015.04.040
CHEMBL3586029 128362 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 530 7 2 8 3.8 C[C@H]1CN(c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)C[C@@H](C)O1 10.1016/j.bmcl.2015.04.040
118709507 120260 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 547 4 2 8 3.8 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc5c(cc4Cl)CCN5C)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319408 120260 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 547 4 2 8 3.8 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc5c(cc4Cl)CCN5C)sc3c2)CC1 10.1021/jm500610n
90666011 116071 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 471 6 0 7 4.7 COc1ccc(-n2cc3nc(-c4ccccc4C)n(CC4CCCN(C(C)C)C4)c(=O)c3n2)cc1 10.1039/C2MD20340E
CHEMBL3218884 116071 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 471 6 0 7 4.7 COc1ccc(-n2cc3nc(-c4ccccc4C)n(CC4CCCN(C(C)C)C4)c(=O)c3n2)cc1 10.1039/C2MD20340E
11538533 81776 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
CHEMBL203280 81776 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
44409998 145314 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 413 7 3 8 2.5 COCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL377515 145314 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 413 7 3 8 2.5 COCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
90666021 116081 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218894 116081 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
11453509 82953 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 441 9 3 7 4.6 COc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL205784 82953 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 441 9 3 7 4.6 COc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
44445610 168502 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 595 11 3 6 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL413608 168502 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 595 11 3 6 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
23648249 85937 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 557 9 4 5 5.4 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1)C1CCNCC1 10.1021/jm0704550
CHEMBL2113326 85937 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 557 9 4 5 5.4 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1)C1CCNCC1 10.1021/jm0704550
11178309 86676 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 445 8 3 7 4.3 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL212415 86676 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 445 8 3 7 4.3 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL3578018 218548 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
CHEMBL3578018 218548 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
44445613 100962 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 512 9 2 5 5.4 O=C(Cc1ccccn1)N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1-c1ccccc1 10.1021/jm701292s
CHEMBL249662 100962 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 512 9 2 5 5.4 O=C(Cc1ccccn1)N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1-c1ccccc1 10.1021/jm701292s
16204229 91092 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
CHEMBL221569 91092 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
44409867 83516 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 473 8 3 7 5.0 CCc1nc(N)nc(Nc2ccccc2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206672 83516 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 473 8 3 7 5.0 CCc1nc(N)nc(Nc2ccccc2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145962494 168853 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160705 168853 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
44389215 69852 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccc(Cl)cc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178838 69852 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccc(Cl)cc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
11211892 86991 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 405 8 3 6 4.0 CC(C)CC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
CHEMBL213703 86991 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 405 8 3 6 4.0 CC(C)CC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
122180015 128354 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 523 9 2 8 5.3 CCCn1cc(-c2cnc(NCc3ccc4occc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586021 128354 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 523 9 2 8 5.3 CCCn1cc(-c2cnc(NCc3ccc4occc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
59446138 88396 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1cccc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163482 88396 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1cccc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
59446138 88396 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1cccc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163482 88396 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1cccc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
59446127 179815 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)N(CCc1ccccc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4518972 179815 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)N(CCc1ccccc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
60195286 88388 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)N(CCc1ccccc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163474 88388 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)N(CCc1ccccc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
10207327 73845 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
CHEMBL18725 73845 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
16112911 91504 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 619 13 4 7 5.6 COc1ccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
CHEMBL222835 91504 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 619 13 4 7 5.6 COc1ccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
5311280 88384 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 1035 25 11 10 2.4 Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)[C@@H]1Cc2cccc3c2N1C(=O)[C@@H](N)CC3)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163470 88384 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 1035 25 11 10 2.4 Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)[C@@H]1Cc2cccc3c2N1C(=O)[C@@H](N)CC3)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44389243 71357 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 557 7 1 6 6.2 O=C(Nc1ccccc1C(=O)N1CCCCC1)c1c(-c2c(Cl)cccc2Cl)noc1CCC1OCCCO1 10.1016/j.bmcl.2004.11.075
CHEMBL181619 71357 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 557 7 1 6 6.2 O=C(Nc1ccccc1C(=O)N1CCCCC1)c1c(-c2c(Cl)cccc2Cl)noc1CCC1OCCCO1 10.1016/j.bmcl.2004.11.075
23648232 98018 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 506 11 3 5 4.5 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/jm0704550
CHEMBL240179 98018 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 506 11 3 5 4.5 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/jm0704550
44445616 168649 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 595 11 3 6 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccncc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL414930 168649 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 595 11 3 6 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccncc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
118709471 120237 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 361 3 2 5 3.9 COc1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319275 120237 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 361 3 2 5 3.9 COc1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
44390889 71197 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 465 8 2 5 2.7 CCN(CC)CCN1C(=O)[C@@](O)(c2cccc(OC)c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL181313 71197 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 465 8 2 5 2.7 CCN(CC)CCN1C(=O)[C@@](O)(c2cccc(OC)c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
46882270 12589 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 7 4 4 4.7 Cc1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078960 12589 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 7 4 4 4.7 Cc1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
156016696 184409 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641201 184409 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL3578016 218546 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
CHEMBL2163348 216103 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163348 216103 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
16113800 144590 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1cccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL375972 144590 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1cccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL3578016 218546 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
156013130 184281 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639514 184281 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156016696 184409 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641201 184409 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145950877 169774 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4175360 169774 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
44358041 168110 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 1724 59 24 24 -8.1 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O)C(C)C 10.1021/jm0001727
91931457 168110 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 1724 59 24 24 -8.1 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O)C(C)C 10.1021/jm0001727
CHEMBL412565 168110 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 1724 59 24 24 -8.1 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O)C(C)C 10.1021/jm0001727
57422810 184440 4 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 602 7 2 10 4.4 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1016/j.bmcl.2020.126953
CHEMBL4641579 184440 4 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 602 7 2 10 4.4 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1016/j.bmcl.2020.126953
16113246 101452 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252643 101452 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
11846624 84691 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 490 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(C1CCCC1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
CHEMBL209443 84691 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 490 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(C1CCCC1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
46882272 12582 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 480 8 4 4 5.5 CC(C)c1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078900 12582 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 480 8 4 4 5.5 CC(C)c1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
9987037 18804 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1183385 18804 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL294324 18804 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
56942537 131978 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 551 12 2 6 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)OCC(C)C)cc1 nan
CHEMBL3645262 131978 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 551 12 2 6 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)OCC(C)C)cc1 nan
57422761 120217 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 510 10 3 8 3.3 COCCNCCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319214 120217 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 510 10 3 8 3.3 COCCNCCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
57422760 120214 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 480 7 2 7 3.6 CN(C)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319211 120214 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 480 7 2 7 3.6 CN(C)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
57422791 120229 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 601 8 2 10 3.5 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cccc(-n5cccn5)c4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319226 120229 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 601 8 2 10 3.5 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cccc(-n5cccn5)c4Cl)sc3c2)CC1 10.1021/jm500610n
44445619 161456 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 541 10 2 5 6.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL399650 161456 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 541 10 2 5 6.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
16113469 144280 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 559 11 4 5 5.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
CHEMBL375408 144280 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 559 11 4 5 5.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
122182045 128778 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 554 9 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCO5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593634 128778 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 554 9 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCO5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
44446175 101762 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 566 13 3 7 4.7 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL254741 101762 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 566 13 3 7 4.7 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
10994861 74045 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 514 9 6 4 2.5 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCNCC1 10.1021/jm020985q
CHEMBL18815 74045 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 514 9 6 4 2.5 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCNCC1 10.1021/jm020985q
10984260 175132 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 529 9 7 5 1.6 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1(N)CCNCC1 10.1021/jm020985q
CHEMBL434391 175132 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 529 9 7 5 1.6 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1(N)CCNCC1 10.1021/jm020985q
59446135 88390 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 859 21 12 9 0.7 NCCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O nan
CHEMBL2163476 88390 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 859 21 12 9 0.7 NCCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O nan
59446135 88390 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 859 21 12 9 0.7 NCCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1021/jm300557t
CHEMBL2163476 88390 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 859 21 12 9 0.7 NCCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1021/jm300557t
59446154 88377 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 858 19 10 8 2.0 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(N)=O nan
CHEMBL2163453 88377 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 858 19 10 8 2.0 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(N)=O nan
59446154 88377 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 858 19 10 8 2.0 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(N)=O 10.1021/jm300557t
CHEMBL2163453 88377 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 858 19 10 8 2.0 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(N)=O 10.1021/jm300557t
44446178 161902 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL402023 161902 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
753168 130017 40 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 349 6 1 4 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL361366 130017 40 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 349 6 1 4 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44338253 16059 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 539 11 1 6 4.4 CN(C)CCCN1C(=O)[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=S 10.1016/j.bmcl.2003.11.012
CHEMBL110900 16059 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 539 11 1 6 4.4 CN(C)CCCN1C(=O)[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=S 10.1016/j.bmcl.2003.11.012
44301512 18794 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 566 13 3 8 1.0 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@@H](N)CO)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1183340 18794 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 566 13 3 8 1.0 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@@H](N)CO)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL291333 18794 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 566 13 3 8 1.0 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@@H](N)CO)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
16113799 175492 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL436849 175492 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
11166495 82325 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 437 8 2 7 4.5 N#Cc1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL204474 82325 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 437 8 2 7 4.5 N#Cc1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
25262772 120242 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 521 6 2 8 2.9 CN1CCN(CCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319281 120242 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 521 6 2 8 2.9 CN1CCN(CCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
44390869 129120 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc(Cl)cc2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL359922 129120 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc(Cl)cc2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
156013130 184281 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639514 184281 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
122180014 128353 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 539 9 2 8 5.8 CCCn1cc(-c2cnc(NCc3ccc4sccc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586020 128353 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 539 9 2 8 5.8 CCCn1cc(-c2cnc(NCc3ccc4sccc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
122178601 128115 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cncc(Br)c2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581034 128115 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cncc(Br)c2)cc1 10.1016/j.bmcl.2014.11.031
16202767 91771 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 506 9 3 5 4.8 Cc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL223810 91771 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 506 9 3 5 4.8 Cc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
46882156 12481 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 404 7 4 4 3.3 CC(C)NC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078115 12481 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 404 7 4 4 3.3 CC(C)NC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
16113474 143411 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 455 8 4 5 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nncn1CCc1c[nH]c2ccccc12 10.1021/jm070024h
CHEMBL373993 143411 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 455 8 4 5 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nncn1CCc1c[nH]c2ccccc12 10.1021/jm070024h
59446105 179600 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)N(Cc1ccc(O)cc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4514053 179600 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)N(Cc1ccc(O)cc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
11556936 88386 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)N(Cc1ccc(O)cc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163472 88386 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)N(Cc1ccc(O)cc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
60195114 88383 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 640 13 8 6 1.8 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm300557t
CHEMBL2163468 88383 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 640 13 8 6 1.8 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm300557t
70690449 82646 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 486 9 0 5 4.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048810 82646 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 486 9 0 5 4.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
70692603 82652 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 463 7 0 5 5.0 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4nc5ccccc5s4)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048816 82652 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 463 7 0 5 5.0 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4nc5ccccc5s4)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
44389192 175425 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 471 4 1 4 6.2 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCCC1 10.1016/j.bmcl.2004.11.075
CHEMBL436275 175425 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 471 4 1 4 6.2 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCCC1 10.1016/j.bmcl.2004.11.075
44394982 72912 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 523 9 1 6 5.7 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL184093 72912 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 523 9 1 6 5.7 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL335799 218343 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0001727
CHEMBL61663 222618 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/s0960-894x(01)00324-9
44445628 168678 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 541 10 2 6 5.5 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL415135 168678 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 541 10 2 6 5.5 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
145950877 169774 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4175360 169774 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
11663710 131245 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 528 9 1 5 6.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL363995 131245 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 528 9 1 5 6.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
16113371 85928 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL2113318 85928 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
16113371 85928 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1021/jm0704550
CHEMBL2113318 85928 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1021/jm0704550
11713497 130015 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 531 9 1 6 6.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)c(C)c1 10.1016/j.bmcl.2004.11.075
CHEMBL361349 130015 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 531 9 1 6 6.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)c(C)c1 10.1016/j.bmcl.2004.11.075
122182045 128778 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 554 9 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCO5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593634 128778 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 554 9 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCO5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
11646276 82709 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
CHEMBL205136 82709 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
122182046 128779 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 586 8 2 6 5.6 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCC3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593635 128779 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 586 8 2 6 5.6 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCC3)cc1Cl 10.1016/j.bmc.2015.05.047
44436828 98775 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 11 4 6 4.3 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL241664 98775 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 11 4 6 4.3 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL410108 219578 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O)C(C)C 10.1021/jm0001727
11538533 81776 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203280 81776 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL500468 220894 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1021/jm020985q
11538534 81789 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
CHEMBL203373 81789 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
122182047 128780 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593636 128780 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
70686293 82658 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 472 5 0 7 3.8 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-c5ncccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048822 82658 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 472 5 0 7 3.8 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-c5ncccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
122180016 128355 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 540 9 2 9 5.1 CCCn1cc(-c2cnc(NCc3ccc4ncsc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586022 128355 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 540 9 2 9 5.1 CCCn1cc(-c2cnc(NCc3ccc4ncsc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
44389216 130632 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 442 6 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C#N)c1 10.1016/j.bmcl.2004.11.075
CHEMBL362595 130632 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 442 6 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C#N)c1 10.1016/j.bmcl.2004.11.075
44389248 128946 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 433 7 2 5 5.0 CCN(CCO)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL359714 128946 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 433 7 2 5 5.0 CCN(CCO)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
145958774 169045 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163811 169045 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
44445609 103814 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 579 10 3 5 6.4 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL266961 103814 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 579 10 3 5 6.4 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
16114532 91471 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccccc1Cn1c(CCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL222610 91471 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccccc1Cn1c(CCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
23648250 85938 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 585 10 4 5 6.0 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
CHEMBL2113327 85938 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 585 10 4 5 6.0 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
44409764 83924 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 488 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL207792 83924 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 488 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44378979 19616 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 506 9 2 5 4.6 NCCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1188586 19616 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 506 9 2 5 4.6 NCCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL536779 19616 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 506 9 2 5 4.6 NCCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
11197 7852 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 10.1016/j.bmcl.2020.126953
154699458 7852 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 10.1016/j.bmcl.2020.126953
CHEMBL4632411 7852 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 10.1016/j.bmcl.2020.126953
CHEMBL498956 220867 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
ChEMBL None None None CCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O)C(C)C 10.1021/jm8014519
46882198 12532 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 460 12 4 4 4.9 CCCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078497 12532 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 460 12 4 4 4.9 CCCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL3578017 218547 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
CHEMBL3578017 218547 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
145953855 169294 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4167669 169294 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
90666035 116095 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 437 6 0 8 2.8 COc1cccc(-n2cc3nc(C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218908 116095 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 437 6 0 8 2.8 COc1cccc(-n2cc3nc(C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
328912 69350 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 505 5 1 4 7.0 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1CC1c2ccccc2CCN1C 10.1016/j.bmcl.2004.11.075
CHEMBL178266 69350 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 505 5 1 4 7.0 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1CC1c2ccccc2CCN1C 10.1016/j.bmcl.2004.11.075
178024 8752 33 None - 1 Human 9.9 pKd = 9.9 Binding
Compound was evaluated for binding affinity using [35S]MK-0677 (800-1100 Ci/mmol), as radioligand having specific high activityCompound was evaluated for binding affinity using [35S]MK-0677 (800-1100 Ci/mmol), as radioligand having specific high activity
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm970342o
5867 8752 33 None - 1 Human 9.9 pKd = 9.9 Binding
Compound was evaluated for binding affinity using [35S]MK-0677 (800-1100 Ci/mmol), as radioligand having specific high activityCompound was evaluated for binding affinity using [35S]MK-0677 (800-1100 Ci/mmol), as radioligand having specific high activity
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm970342o
CHEMBL13817 8752 33 None - 1 Human 9.9 pKd = 9.9 Binding
Compound was evaluated for binding affinity using [35S]MK-0677 (800-1100 Ci/mmol), as radioligand having specific high activityCompound was evaluated for binding affinity using [35S]MK-0677 (800-1100 Ci/mmol), as radioligand having specific high activity
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm970342o
57398340 78051 0 None - 1 Human 11.0 pKi = 11 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 449 5 0 8 4.6 Cc1nc2ccc(Oc3ccc4ncsc4c3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956993 78051 0 None - 1 Human 11.0 pKi = 11 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 449 5 0 8 4.6 Cc1nc2ccc(Oc3ccc4ncsc4c3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57400002 78052 0 None - 1 Human 11.0 pKi = 11 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 488 5 0 6 4.9 Cc1nc2ccc(Oc3ccc(Br)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956994 78052 0 None - 1 Human 11.0 pKi = 11 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 488 5 0 6 4.9 Cc1nc2ccc(Oc3ccc(Br)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57394881 78068 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 489 5 0 7 4.3 Cc1nc2ncc(Oc3ccc(Br)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957010 78068 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 489 5 0 7 4.3 Cc1nc2ncc(Oc3ccc(Br)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57393073 78059 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 449 5 0 8 4.6 Cc1nc2cnc(Oc3ccc4ncsc4c3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957001 78059 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 449 5 0 8 4.6 Cc1nc2cnc(Oc3ccc4ncsc4c3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
56926461 75811 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923609 75811 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926462 75812 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923610 75812 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
56926680 75825 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccccc2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923623 75825 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccccc2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
56926682 75827 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923625 75827 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
11664206 75828 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923626 75828 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
56926893 75838 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 nan
CHEMBL1923637 75838 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 nan
11526745 75843 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923642 75843 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134137202 149604 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 5 3 6 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3893048 149604 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 5 3 6 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134137257 149915 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 540 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3895776 149915 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 540 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134133352 150283 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3898794 150283 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@@H](C)N(C)C1=O nan
11527086 150828 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 574 3 3 5 3.4 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)c(Cl)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3903118 150828 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 574 3 3 5 3.4 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)c(Cl)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
11512561 151147 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 574 3 3 5 3.4 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2Cl)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3905791 151147 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 574 3 3 5 3.4 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2Cl)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134133037 151345 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3907497 151345 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](C)N(C)C1=O nan
134132670 151392 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3907891 151392 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134132152 151710 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3910300 151710 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@@H](C)N(C)C1=O nan
134142839 152164 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3913855 152164 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134142553 152225 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3914259 152225 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134143635 152352 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2Cl)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3915269 152352 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2Cl)NC(=O)C2(CCCC2)NC1=O nan
134143096 152711 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 584 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2ccc(Br)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3918009 152711 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 584 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2ccc(Br)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134142204 152715 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3918046 152715 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
11584702 152969 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 540 3 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3920049 152969 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 540 3 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134139279 153225 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 594 4 4 5 4.1 CCC(C)[C@H]1NCCOc2ccccc2[C@H]2C[C@@H]2CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3922056 153225 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 594 4 4 5 4.1 CCC(C)[C@H]1NCCOc2ccccc2[C@H]2C[C@@H]2CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134138445 154155 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NC/C=C/c2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3929593 154155 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NC/C=C/c2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134138218 154788 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NC/C=C\c2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3934367 154788 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NC/C=C\c2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134148686 154950 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3935670 154950 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134149719 155466 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 2 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C(C)(C)C)C(=O)N1C nan
CHEMBL3939872 155466 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 2 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C(C)(C)C)C(=O)N1C nan
134145791 155565 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2c(F)c(F)c(F)c(F)c2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3940705 155565 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2c(F)c(F)c(F)c(F)c2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134143746 157379 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 2 4 5 3.9 O=C1NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1cccc(Cl)c1 nan
CHEMBL3955179 157379 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 2 4 5 3.9 O=C1NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1cccc(Cl)c1 nan
134145221 157411 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CCC(C)C1NC[C@H](C)Oc2ccccc2CCCNC(=O)C(Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3955437 157411 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CCC(C)C1NC[C@H](C)Oc2ccccc2CCCNC(=O)C(Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134155656 157973 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3959816 157973 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@@H](C)N(C)C1=O nan
134155282 158121 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3961108 158121 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134153496 159064 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 3 5 2.4 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3969367 159064 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 3 5 2.4 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134153654 159545 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 632 3 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(I)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3973513 159545 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 632 3 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(I)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134157569 160815 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 560 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2cc(F)c(F)c(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3984338 160815 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 560 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2cc(F)c(F)c(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
57345600 78048 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 488 5 0 6 4.9 Cc1nc2ncc(Oc3ccc(Br)cc3F)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956990 78048 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 488 5 0 6 4.9 Cc1nc2ncc(Oc3ccc(Br)cc3F)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57345599 78049 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 444 5 0 6 4.8 Cc1nc2ccc(Oc3ccc(Cl)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956991 78049 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 444 5 0 6 4.8 Cc1nc2ccc(Oc3ccc(Cl)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57398341 78057 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 444 5 0 6 4.8 Cc1nc2cnc(Oc3ccc(Cl)cc3F)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956999 78057 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 444 5 0 6 4.8 Cc1nc2cnc(Oc3ccc(Cl)cc3F)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
178024 8752 33 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm960054c
5867 8752 33 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm960054c
CHEMBL13817 8752 33 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm960054c
57398342 78065 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 450 5 0 9 4.0 Cc1nc2ncc(Oc3ccc4ncsc4c3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957007 78065 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 450 5 0 9 4.0 Cc1nc2ncc(Oc3ccc4ncsc4c3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57401803 78067 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 469 6 0 7 5.1 Cc1nc2ncc(Oc3ccc(-c4ccccc4)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957009 78067 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 469 6 0 7 5.1 Cc1nc2ncc(Oc3ccc(-c4ccccc4)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57401799 78058 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 436 5 0 8 3.7 Cc1nc2cnc(Oc3ccc4c(c3)OCO4)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957000 78058 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 436 5 0 8 3.7 Cc1nc2cnc(Oc3ccc4c(c3)OCO4)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57399248 75819 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923617 75819 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
44340008 120165 0 None - 1 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 583 9 2 6 3.2 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)c(F)c1)C(=O)N1CCC2=NN(C(C)(C)C)C(=O)C2(Cc2ccccc2)C1 10.1016/s0960-894x(02)00734-5
CHEMBL331801 120165 0 None - 1 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 583 9 2 6 3.2 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)c(F)c1)C(=O)N1CCC2=NN(C(C)(C)C)C(=O)C2(Cc2ccccc2)C1 10.1016/s0960-894x(02)00734-5
57399248 75819 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923617 75819 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
24970113 75831 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 580 3 3 5 3.8 C[C@@H]1CN[C@@H](C2CCCCC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923629 75831 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 580 3 3 5 3.8 C[C@@H]1CN[C@@H](C2CCCCC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
57391293 78055 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 468 6 0 6 5.7 Cc1nc2ccc(Oc3ccc(-c4ccccc4)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956997 78055 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 468 6 0 6 5.7 Cc1nc2ccc(Oc3ccc(-c4ccccc4)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
162659411 188004 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 575 13 3 7 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CC#N)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4761419 188004 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 575 13 3 7 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CC#N)cc1 10.1021/acs.jmedchem.9b02122
44340268 117298 0 None - 1 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 609 10 2 6 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)c(F)c1)C(=O)N1CCC2=NN(CC(F)(F)F)C(=O)C2(Cc2ccccc2)C1 10.1016/s0960-894x(02)00734-5
CHEMBL325062 117298 0 None - 1 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 609 10 2 6 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)c(F)c1)C(=O)N1CCC2=NN(CC(F)(F)F)C(=O)C2(Cc2ccccc2)C1 10.1016/s0960-894x(02)00734-5
57401800 78061 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 446 5 0 8 3.9 Cc1nc2cnc(Oc3ccc4c(c3)ncn4C)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957003 78061 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 446 5 0 8 3.9 Cc1nc2cnc(Oc3ccc4c(c3)ncn4C)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
162657606 187896 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 693 15 3 8 5.7 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4760409 187896 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 693 15 3 8 5.7 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
57401801 78063 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 445 5 0 7 4.2 Cc1nc2ncc(Oc3ccc(Cl)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957005 78063 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 445 5 0 7 4.2 Cc1nc2ncc(Oc3ccc(Cl)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
162672839 189801 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 681 14 3 7 5.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4793824 189801 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 681 14 3 7 5.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL500468 220894 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1021/jm300414b
56942242 131973 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645257 131973 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 10.1016/j.bmcl.2016.04.003
56925343 75841 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 550 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cccc3c2O[C@H](CC3)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923640 75841 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 550 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cccc3c2O[C@H](CC3)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
57398339 78050 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 436 5 0 8 3.7 Cc1nc2ccc(Oc3ccc4c(c3)OCO4)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956992 78050 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 436 5 0 8 3.7 Cc1nc2ccc(Oc3ccc4c(c3)OCO4)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
162645413 186505 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 677 14 3 7 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4744051 186505 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 677 14 3 7 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(C)cc2)cc1 10.1021/acs.jmedchem.9b02122
155540883 179736 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4517399 179736 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
16133832 220110 18 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/acs.jmedchem.8b01644
CHEMBL425281 220110 18 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/acs.jmedchem.8b01644
162653781 187261 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 732 15 4 8 6.2 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3c[nH]c4ccccc34)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4753046 187261 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 732 15 4 8 6.2 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3c[nH]c4ccccc34)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
57401802 78064 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 437 5 0 9 3.1 Cc1nc2ncc(Oc3ccc4c(c3)OCO4)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957006 78064 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 437 5 0 9 3.1 Cc1nc2ncc(Oc3ccc4c(c3)OCO4)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57401797 78044 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 468 6 0 6 5.7 Cc1nc2ncc(Oc3ccc(-c4ccccc4)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956987 78044 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 468 6 0 6 5.7 Cc1nc2ncc(Oc3ccc(-c4ccccc4)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57398343 78066 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 462 5 0 8 4.1 Cc1nc2ncc(Oc3ccc(F)c4cccnc34)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957008 78066 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 462 5 0 8 4.1 Cc1nc2ncc(Oc3ccc(F)c4cccnc34)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
56926175 75788 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL1923504 75788 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
56926360 75810 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 4 3 5 2.7 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923608 75810 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 4 3 5 2.7 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926582 75818 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](CCc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923616 75818 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](CCc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926681 75826 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2cccc(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923624 75826 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2cccc(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
56926891 75836 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923635 75836 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926892 75837 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923636 75837 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926894 75839 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
CHEMBL1923638 75839 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
56925345 75844 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(F)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923643 75844 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(F)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134130631 149151 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 576 5 4 6 3.4 COc1ccc(C[C@@H]2NC(=O)C3(CCCC3)NC(=O)[C@H](CC(C)C)NCCOc3ccccc3/C=C\CNC2=O)cc1 nan
CHEMBL3889512 149151 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 576 5 4 6 3.4 COc1ccc(C[C@@H]2NC(=O)C3(CCCC3)NC(=O)[C@H](CC(C)C)NCCOc3ccccc3/C=C\CNC2=O)cc1 nan
134131442 149174 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3889678 149174 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134131183 149246 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3890296 149246 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134136433 149285 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 576 5 4 6 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(OC)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3890602 149285 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 576 5 4 6 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(OC)c2)NC(=O)C2(CCCC2)NC1=O nan
134137008 149321 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 4 4 5 3.5 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(F)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3890889 149321 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 4 4 5 3.5 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(F)c2)NC(=O)C2(CCCC2)NC1=O nan
134137012 149380 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 512 3 3 6 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccsc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3891381 149380 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 512 3 3 6 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccsc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134137398 149654 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 594 4 4 4 4.9 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3893476 149654 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 594 4 4 4 4.9 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134136665 149677 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 630 4 5 6 3.9 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2cccc(Cl)c2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccc(O)cc1 nan
CHEMBL3893697 149677 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 630 4 5 6 3.9 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2cccc(Cl)c2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccc(O)cc1 nan
134133488 150014 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 600 4 4 5 4.1 CC[C@H](C)[C@@H]1NCCOc2ccc(F)cc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3896536 150014 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 600 4 4 5 4.1 CC[C@H](C)[C@@H]1NCCOc2ccc(F)cc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134134248 150129 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 598 5 3 5 4.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](C(c2ccccc2)c2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3897510 150129 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 598 5 3 5 4.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](C(c2ccccc2)c2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134134556 150130 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 3 4 5 2.7 CC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3897527 150130 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 3 4 5 2.7 CC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134133518 150231 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 2 4 5 3.4 CC1(C)NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
CHEMBL3898348 150231 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 2 4 5 3.4 CC1(C)NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
134134286 150472 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 598 5 3 5 4.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3900284 150472 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 598 5 3 5 4.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134135296 150789 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 3 4 5 3.0 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3902856 150789 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 3 4 5 3.0 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134132958 151439 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 3 3 5 2.4 C[C@H]1C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)NC[C@H]2C[C@@H]2c2ccccc2OCCN[C@H](C2CC2)C(=O)N1C nan
CHEMBL3908264 151439 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 3 3 5 2.4 C[C@H]1C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)NC[C@H]2C[C@@H]2c2ccccc2OCCN[C@H](C2CC2)C(=O)N1C nan
134132137 151591 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 4 3 4 3.5 CCC(C)C1NCCCc2ccccc2/C=C\CNC(=O)C(Cc2ccc(F)cc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3909431 151591 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 4 3 4 3.5 CCC(C)C1NCCCc2ccccc2/C=C\CNC(=O)C(Cc2ccc(F)cc2)NC(=O)C(C)N(C)C1=O nan
134132893 151641 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 4 4 6 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3909834 151641 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 4 4 6 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
24969783 151642 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccc(F)cc2O1 nan
CHEMBL3909838 151642 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccc(F)cc2O1 nan
130334810 151938 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 2 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)N2CC[C@@H](C2=O)N(C)C1=O nan
CHEMBL3912211 151938 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 2 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)N2CC[C@@H](C2=O)N(C)C1=O nan
134132394 151962 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 523 4 3 6 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccn2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3912375 151962 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 523 4 3 6 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccn2)NC(=O)[C@@H](C)N(C)C1=O nan
134142218 152065 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 4 4 5 3.5 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3913052 152065 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 4 4 5 3.5 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)C2(CCCC2)NC1=O nan
134142433 152104 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 3 4 6 1.8 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOC2)NC1=O nan
CHEMBL3913335 152104 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 3 4 6 1.8 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOC2)NC1=O nan
59778970 152153 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 4 3 6 1.8 COC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3913763 152153 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 4 3 6 1.8 COC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134143366 152538 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 4 4 4 4.6 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3916659 152538 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 4 4 4 4.6 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
117812386 152636 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NC/C=C\c2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3917385 152636 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NC/C=C\c2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134139489 152840 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2cc(F)cc(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3919021 152840 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2cc(F)cc(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134140270 153151 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 4 3 5 3.1 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3921499 153151 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 4 3 5 3.1 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134140007 153182 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)c(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3921750 153182 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)c(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134139286 153332 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3922810 153332 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
134139113 153431 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CC)N(C)C1=O nan
CHEMBL3923633 153431 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CC)N(C)C1=O nan
134141159 153507 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 523 4 3 6 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3924192 153507 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 523 4 3 6 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](C)N(C)C1=O nan
134140968 153568 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 3 3 5 2.4 CC1C(=O)NC(Cc2ccc(F)cc2)C(=O)NC[C@H]2C[C@@H]2c2ccccc2OCCNC(C2CC2)C(=O)N1C nan
CHEMBL3924635 153568 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 3 3 5 2.4 CC1C(=O)NC(Cc2ccc(F)cc2)C(=O)NC[C@H]2C[C@@H]2c2ccccc2OCCNC(C2CC2)C(=O)N1C nan
134141782 153772 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 4 4 4 4.6 CCC(C)C1NCCCc2ccccc2/C=C\CNC(=O)C(Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3926434 153772 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 4 4 4 4.6 CCC(C)C1NCCCc2ccccc2/C=C\CNC(=O)C(Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134141886 153896 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 546 4 4 5 3.4 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3927481 153896 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 546 4 4 5 3.4 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134138234 154191 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 3 3 5 2.4 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccc3c(c2)OC(CC3)CN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3929852 154191 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 3 3 5 2.4 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccc3c(c2)OC(CC3)CN[C@@H](C2CC2)C(=O)N1C nan
117812380 154530 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 617 5 4 7 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(NS(C)(=O)=O)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3932408 154530 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 617 5 4 7 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(NS(C)(=O)=O)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134138595 154533 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 544 2 4 5 3.3 O=C1NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccccc1 nan
CHEMBL3932434 154533 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 544 2 4 5 3.3 O=C1NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccccc1 nan
134138824 154793 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 525 3 3 6 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ncccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3934402 154793 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 525 3 3 6 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ncccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134148504 155133 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 4 3 4 3.4 CC[C@H](C)[C@@H]1NCc2ccccc2C/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3937200 155133 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 4 3 4 3.4 CC[C@H](C)[C@@H]1NCc2ccccc2C/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134149092 155232 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 4 5 2.5 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O nan
CHEMBL3937924 155232 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 4 5 2.5 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O nan
134149306 155253 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 3 3 5 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCC#Cc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3938104 155253 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 3 3 5 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCC#Cc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134149407 155299 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 571 4 4 6 3.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(C#N)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3938452 155299 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 571 4 4 6 3.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(C#N)c2)NC(=O)C2(CCCC2)NC1=O nan
134148639 155322 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 583 4 5 6 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCNC2)NC1=O nan
CHEMBL3938683 155322 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 583 4 5 6 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCNC2)NC1=O nan
134146570 155559 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3940653 155559 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134145552 155798 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(CC)C1=O nan
CHEMBL3942528 155798 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(CC)C1=O nan
134145564 155869 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3943086 155869 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
72574018 155883 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CCC(C)C1NCC(C)Oc2ccccc2CCCNC(=O)C(Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3943159 155883 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CCC(C)C1NCC(C)Oc2ccccc2CCCNC(=O)C(Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134146319 155905 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2CC(C)CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3943294 155905 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2CC(C)CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134147809 156228 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 546 4 4 5 3.4 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3946007 156228 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 546 4 4 5 3.4 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134147441 156268 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 2 4 5 3.0 C[C@H]1NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
CHEMBL3946348 156268 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 2 4 5 3.0 C[C@H]1NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
134146888 156542 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 624 4 4 5 4.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Br)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3948268 156542 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 624 4 4 5 4.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Br)c2)NC(=O)C2(CCCC2)NC1=O nan
134147381 156564 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 546 4 4 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3948472 156564 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 546 4 4 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134147802 156870 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.6 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cc(F)cc(F)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3950904 156870 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.6 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cc(F)cc(F)c2)NC(=O)C2(CCCC2)NC1=O nan
134145064 156929 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 2 4 5 3.4 CC1(C)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3951476 156929 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 2 4 5 3.4 CC1(C)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134144205 157053 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(C(F)(F)F)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3952596 157053 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(C(F)(F)F)c2)NC(=O)C2(CCCC2)NC1=O nan
134144429 157065 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3952699 157065 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134144211 157110 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 4 4 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2C#CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3953033 157110 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 4 4 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2C#CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134144606 157114 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.5 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3953053 157114 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.5 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)C2(CCCC2)NC1=O nan
134155024 157791 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 4 3.6 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3958451 157791 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 4 3.6 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134155239 157793 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 3 4 5 3.4 O=C1NC/C=C\c2ccccc2OCCN[C@@H](C2CC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccc(Cl)cc1 nan
CHEMBL3958460 157793 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 3 4 5 3.4 O=C1NC/C=C\c2ccccc2OCCN[C@@H](C2CC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccc(Cl)cc1 nan
134155132 157871 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 502 4 3 5 2.9 CC[C@H](C)[C@]1(C)NCCOc2ccccc2CCCNC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3959108 157871 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 502 4 3 5 2.9 CC[C@H](C)[C@]1(C)NCCOc2ccccc2CCCNC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](C)N(C)C1=O nan
134155178 158158 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 525 3 3 6 1.6 CC1C(=O)NC(Cc2ccc(F)cc2)C(=O)NCCCc2ncccc2OCCNC(C2CC2)C(=O)N1C nan
CHEMBL3961456 158158 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 525 3 3 6 1.6 CC1C(=O)NC(Cc2ccc(F)cc2)C(=O)NCCCc2ncccc2OCCNC(C2CC2)C(=O)N1C nan
134150646 158425 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 558 5 3 6 2.6 CSCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3963865 158425 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 558 5 3 6 2.6 CSCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134150029 158894 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 4 3 4 3.3 CC[C@H](C)C1NCCCc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3967783 158894 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 4 3 4 3.3 CC[C@H](C)C1NCCCc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
134150729 158935 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 3 3 5 2.1 CC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3968175 158935 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 3 3 5 2.1 CC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134154254 159078 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 4 3 4 3.5 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3969506 159078 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 4 3 4 3.5 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134154486 159221 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 2 3 5 3.3 C[C@@H]1C(=O)N[C@H](Cc2cccc(Cl)c2)C(=O)NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)N1C nan
CHEMBL3970827 159221 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 2 3 5 3.3 C[C@@H]1C(=O)N[C@H](Cc2cccc(Cl)c2)C(=O)NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)N1C nan
134154392 159311 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 4 4 5 3.1 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3971540 159311 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 4 4 5 3.1 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134153247 159499 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 6 2.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCOC2)NC1=O nan
CHEMBL3973085 159499 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 6 2.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCOC2)NC1=O nan
134153772 159678 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 528 4 3 6 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccs2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3974701 159678 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 528 4 3 6 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccs2)NC(=O)[C@@H](C)N(C)C1=O nan
52911621 159840 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 531 3 3 6 1.9 C[C@@H]1C(=O)N[C@H](Cc2ccc(C#N)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3975975 159840 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 531 3 3 6 1.9 C[C@@H]1C(=O)N[C@H](Cc2ccc(C#N)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134151758 159883 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 558 3 3 5 2.9 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(Cl)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3976294 159883 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 558 3 3 5 2.9 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(Cl)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134152984 159947 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 6 2.9 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2ccc(Cl)cc2)NC(=O)C2(CCOC2)NC1=O nan
CHEMBL3976853 159947 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 6 2.9 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2ccc(Cl)cc2)NC(=O)C2(CCOC2)NC1=O nan
134151899 160098 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3978207 160098 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
134152339 160238 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 545 3 4 5 2.6 C[C@@H]1C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3979468 160238 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 545 3 4 5 2.6 C[C@@H]1C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134152133 160302 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 3 4 6 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(O)c(C(C)(C)C)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3979911 160302 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 3 4 6 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(O)c(C(C)(C)C)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134157813 160451 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 524 4 3 6 1.7 COC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3981238 160451 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 524 4 3 6 1.7 COC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134156963 160637 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.5 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3982825 160637 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.5 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)C2(CCCC2)NC1=O nan
57528321 160736 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 2 2 5 2.6 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN2CCCC[C@H]2C(=O)N1C nan
CHEMBL3983626 160736 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 2 2 5 2.6 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN2CCCC[C@H]2C(=O)N1C nan
134156579 160833 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.6 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(F)c(F)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3984464 160833 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.6 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(F)c(F)c2)NC(=O)C2(CCCC2)NC1=O nan
134156405 161041 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 620 4 4 6 4.3 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccsc1 nan
CHEMBL3986375 161041 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 620 4 4 6 4.3 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccsc1 nan
134156453 161079 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 523 4 3 6 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccncc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3986628 161079 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 523 4 3 6 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccncc2)NC(=O)[C@@H](C)N(C)C1=O nan
56942098 131971 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645255 131971 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
162646324 186515 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 688 17 3 9 4.8 CCN(CC)CCc1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(OC)cc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4744139 186515 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 688 17 3 9 4.8 CCN(CC)CCc1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(OC)cc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
162665018 188914 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 550 12 3 6 4.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(C)=O)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4782214 188914 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 550 12 3 6 4.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(C)=O)cc1 10.1021/acs.jmedchem.9b02122
58438451 99060 0 None 2089 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 442 4 0 6 3.1 Cc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426689 99060 0 None 2089 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 442 4 0 6 3.1 Cc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
90644553 118512 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 540 5 1 7 4.0 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN([C@@H]3CCc5cc(-c6ccc(C(N)=O)nc6)ccc53)C4)nc2s1 10.1021/ml400473x
CHEMBL3287214 118512 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 540 5 1 7 4.0 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN([C@@H]3CCc5cc(-c6ccc(C(N)=O)nc6)ccc53)C4)nc2s1 10.1021/ml400473x
56926177 75790 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL1923506 75790 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
56926268 75792 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 4 3 5 2.5 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](Cc2ccccc2)C1=O nan
CHEMBL1923510 75792 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 4 3 5 2.5 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](Cc2ccccc2)C1=O nan
56926269 75793 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 460 5 3 5 2.0 CCCC[C@H]1NC(=O)CN(C)C(=O)[C@H](CCC)NCCOc2ccccc2CCCNC1=O nan
CHEMBL1923511 75793 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 460 5 3 5 2.0 CCCC[C@H]1NC(=O)CN(C)C(=O)[C@H](CCC)NCCOc2ccccc2CCCNC1=O nan
56926356 75794 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O nan
CHEMBL1923512 75794 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O nan
56926465 75815 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 4 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
CHEMBL1923613 75815 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 4 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
56926782 75832 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 472 4 3 4 3.0 CC[C@H](C)[C@@H]1NCCCCCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923631 75832 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 472 4 3 4 3.0 CC[C@H](C)[C@@H]1NCCCCCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926784 75834 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 4 2.9 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923633 75834 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 4 2.9 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926785 75835 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923634 75835 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
71452183 90304 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 5 4 6 1.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)N(C)C1=O nan
CHEMBL2203623 90304 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 5 4 6 1.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)N(C)C1=O nan
134131439 149173 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 527 4 4 6 1.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CCN)C(=O)N1C nan
CHEMBL3889672 149173 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 527 4 4 6 1.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CCN)C(=O)N1C nan
134137460 149413 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 4 5 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
CHEMBL3891657 149413 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 4 5 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
134136637 149498 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 541 5 4 6 1.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CCCN)C(=O)N1C nan
CHEMBL3892319 149498 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 541 5 4 6 1.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CCCN)C(=O)N1C nan
134136946 149532 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 566 5 4 6 2.4 CC[C@H](C)[C@@H]1NCCOc2ccc(C(=O)O)cc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3892517 149532 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 566 5 4 6 2.4 CC[C@H](C)[C@@H]1NCCOc2ccc(C(=O)O)cc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134136405 149697 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 616 4 4 5 4.6 CC[C@H](C)[C@@H]1NCCOc2ccc(Cl)cc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3893850 149697 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 616 4 4 5 4.6 CC[C@H](C)[C@@H]1NCCOc2ccc(Cl)cc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134133771 150119 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 474 4 3 5 2.3 CCC[C@H]1NC(=O)[C@@H](C)N(C)C(=O)[C@H]([C@@H](C)CC)NCCOc2ccccc2CCCNC1=O nan
CHEMBL3897387 150119 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 474 4 3 5 2.3 CCC[C@H]1NC(=O)[C@@H](C)N(C)C(=O)[C@H]([C@@H](C)CC)NCCOc2ccccc2CCCNC1=O nan
134133353 150297 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 550 5 3 5 3.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)N(C)C1=O nan
CHEMBL3898864 150297 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 550 5 3 5 3.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)N(C)C1=O nan
134134505 150446 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 4 4 4 4.3 CC[C@H](C)[C@@H]1NCCCCCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3900035 150446 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 4 4 4 4.3 CC[C@H](C)[C@@H]1NCCCCCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134134605 150455 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 474 3 3 5 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](C(C)C)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3900122 150455 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 474 3 3 5 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](C(C)C)NC(=O)[C@@H](C)N(C)C1=O nan
134134099 150509 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 639 4 4 6 4.1 N#Cc1ccccc1C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3900636 150509 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 639 4 4 6 4.1 N#Cc1ccccc1C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
134135897 150772 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 530 4 4 4 4.0 CC[C@H](C)[C@@H]1NCCCC/C=C/CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3902804 150772 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 530 4 4 4 4.0 CC[C@H](C)[C@@H]1NCCCC/C=C/CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134134825 150857 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 476 3 3 5 1.4 C[C@@H]1C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)NCCCCCOCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3903351 150857 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 476 3 3 5 1.4 C[C@@H]1C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)NCCCCCOCCN[C@@H](C2CC2)C(=O)N1C nan
72989837 150893 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 5 4 6 1.7 CCC(C)C1NCCOc2ccccc2CCCNC(=O)C(Cc2ccccc2)NC(=O)C(CO)N(C)C1=O nan
CHEMBL3903647 150893 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 5 4 6 1.7 CCC(C)C1NCCOc2ccccc2CCCNC(=O)C(Cc2ccccc2)NC(=O)C(CO)N(C)C1=O nan
134135712 150916 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 533 4 4 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN(C)C1=O nan
CHEMBL3903845 150916 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 533 4 4 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN(C)C1=O nan
134136025 151110 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 550 6 4 6 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](COCc2ccccc2)NC(=O)C(C)(C)NC1=O nan
CHEMBL3905495 151110 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 550 6 4 6 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](COCc2ccccc2)NC(=O)C(C)(C)NC1=O nan
134134870 151170 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 3 4 5 2.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3905987 151170 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 3 4 5 2.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134135261 151263 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC)N(C)C1=O nan
CHEMBL3906788 151263 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC)N(C)C1=O nan
134134893 151289 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 2 3 5 3.3 C[C@H]1C(=O)N[C@H](Cc2cccc(Cl)c2)C(=O)NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)N1C nan
CHEMBL3907031 151289 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 2 3 5 3.3 C[C@H]1C(=O)N[C@H](Cc2cccc(Cl)c2)C(=O)NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)N1C nan
134132666 151343 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 583 4 4 6 3.3 CC[C@H](C)[C@@H]1NCCOc2cccnc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3907480 151343 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 583 4 4 6 3.3 CC[C@H](C)[C@@H]1NCCOc2cccnc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134132519 151427 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 4 4 6 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccsc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3908156 151427 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 4 4 6 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccsc2)NC(=O)C2(CCCC2)NC1=O nan
134132427 151479 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 622 5 4 5 5.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3908583 151479 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 622 5 4 5 5.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)C2(CCCC2)NC1=O nan
134131971 151706 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.5 CC[C@H](C)[C@@H]1NCCOc2ccccc2C(C)CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3910288 151706 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.5 CC[C@H](C)[C@@H]1NCCOc2ccccc2C(C)CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134132265 151749 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 548 3 4 6 2.2 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOCC2)NC1=O nan
CHEMBL3910661 151749 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 548 3 4 6 2.2 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOCC2)NC1=O nan
134131903 151916 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 529 4 3 7 2.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cscn2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3912034 151916 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 529 4 3 7 2.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cscn2)NC(=O)[C@@H](C)N(C)C1=O nan
134132099 151988 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 4 4 6 3.4 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccs2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3912534 151988 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 4 4 6 3.4 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccs2)NC(=O)C2(CCCC2)NC1=O nan
134142223 152121 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 480 4 4 5 1.7 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CNC1=O nan
CHEMBL3913486 152121 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 480 4 4 5 1.7 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CNC1=O nan
134142139 152180 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 610 5 4 6 3.6 COc1ccc(C[C@@H]2NCCOc3ccccc3/C=C\CNC(=O)[C@H](Cc3ccccc3)NC(=O)C3(CCCC3)NC2=O)cc1 nan
CHEMBL3913981 152180 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 610 5 4 6 3.6 COc1ccc(C[C@@H]2NCCOc3ccccc3/C=C\CNC(=O)[C@H](Cc3ccccc3)NC(=O)C3(CCCC3)NC2=O)cc1 nan
76460236 152238 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 472 4 3 4 3.0 CCC(C)C1NCCCCCCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3914338 152238 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 472 4 3 4 3.0 CCC(C)C1NCCCCCCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
134143044 152251 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 488 4 3 5 2.5 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H]([C@@H](C)CC)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3914467 152251 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 488 4 3 5 2.5 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H]([C@@H](C)CC)NC(=O)[C@@H](C)N(C)C1=O nan
134143657 152514 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 528 4 3 6 1.4 COC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3916501 152514 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 528 4 3 6 1.4 COC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134143398 152712 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 3 3 5 2.9 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCC(C)(C)c2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3918022 152712 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 3 3 5 2.9 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCC(C)(C)c2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134139992 153117 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.2 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccccc1Cl nan
CHEMBL3921227 153117 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.2 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccccc1Cl nan
134140213 153398 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 513 3 4 6 0.8 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CN)C(=O)N1C nan
CHEMBL3923324 153398 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 513 3 4 6 0.8 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CN)C(=O)N1C nan
134140762 153443 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 505 4 2 5 3.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)N2CC[C@@H](C1=O)C2=O nan
CHEMBL3923718 153443 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 505 4 2 5 3.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)N2CC[C@@H](C1=O)C2=O nan
134141057 153473 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 3 4 5 2.7 CCC1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3923918 153473 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 3 4 5 2.7 CCC1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134140844 154003 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.2 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1cccc(Cl)c1 nan
CHEMBL3928367 154003 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.2 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1cccc(Cl)c1 nan
68186750 154165 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.8 CC1CCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)NCCOc2ccccc21 nan
CHEMBL3929656 154165 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.8 CC1CCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)NCCOc2ccccc21 nan
134138656 154332 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 504 4 3 4 3.0 CC[C@H](C)[C@@H]1NCCc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3930811 154332 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 504 4 3 4 3.0 CC[C@H](C)[C@@H]1NCCc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134138764 154414 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 566 5 3 7 2.1 COc1ccc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NCCOc3ccccc3CCCNC2=O)cc1OC nan
CHEMBL3931402 154414 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 566 5 3 7 2.1 COc1ccc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NCCOc3ccccc3CCCNC2=O)cc1OC nan
134138160 154443 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 512 4 4 6 1.4 CCC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3931716 154443 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 512 4 4 6 1.4 CCC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H](C)N(C)C1=O nan
134137758 154752 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 500 7 4 5 3.2 CCCC[C@@H]1NC(=O)[C@H](CCCC)NC(=O)[C@@H](C(C)C)NCCOc2ccccc2/C=C\CNC1=O nan
CHEMBL3934093 154752 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 500 7 4 5 3.2 CCCC[C@@H]1NC(=O)[C@H](CCCC)NC(=O)[C@@H](C(C)C)NCCOc2ccccc2/C=C\CNC1=O nan
134137945 154764 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 3 4 5 3.2 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(Cc3ccccc3C2)NC1=O nan
CHEMBL3934184 154764 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 3 4 5 3.2 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(Cc3ccccc3C2)NC1=O nan
134149048 154855 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 3 5 6 1.2 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@H]1CO nan
CHEMBL3934901 154855 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 3 5 6 1.2 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@H]1CO nan
134149058 154913 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 586 4 4 6 3.6 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1cccs1 nan
CHEMBL3935422 154913 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 586 4 4 6 3.6 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1cccs1 nan
134149451 154944 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCCc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3935626 154944 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCCc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134148804 155097 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 3 4 6 2.9 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCSCC2)NC1=O nan
CHEMBL3936957 155097 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 3 4 6 2.9 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCSCC2)NC1=O nan
58012657 155144 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 544 4 3 5 3.9 CCC[C@@H]1NCc2ccccc2Sc2ccccc2CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3937314 155144 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 544 4 3 5 3.9 CCC[C@@H]1NCc2ccccc2Sc2ccccc2CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
134149772 155258 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 592 4 4 4 5.0 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3938132 155258 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 592 4 4 4 5.0 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134149793 155384 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 5 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(CC)C1=O nan
CHEMBL3939196 155384 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 5 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(CC)C1=O nan
134148754 155478 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 646 8 3 6 4.0 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C(COCc2ccccc2)N(C)C1=O nan
CHEMBL3939993 155478 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 646 8 3 6 4.0 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)C(COCc2ccccc2)N(C)C1=O nan
134145258 155581 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 4 4.8 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3940860 155581 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 4 4.8 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134145652 155802 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 576 6 4 6 3.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](COCc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3942543 155802 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 576 6 4 6 3.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](COCc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134145920 155805 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 2 4 5 2.3 C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3942554 155805 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 2 4 5 2.3 C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134146710 155809 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 587 4 4 7 3.0 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1cscn1 nan
CHEMBL3942610 155809 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 587 4 4 7 3.0 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1cscn1 nan
134145820 155813 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 4 2.9 CC[C@H](C)[C@@H]1NCCc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3942642 155813 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 4 2.9 CC[C@H](C)[C@@H]1NCCc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134146617 155894 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 4 5 3.0 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3943228 155894 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 4 5 3.0 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134145420 156092 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 6 3 5 3.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)N(C)C1=O nan
CHEMBL3944936 156092 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 6 3 5 3.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)N(C)C1=O nan
134147617 156214 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)C(C)(C)NC1=O nan
CHEMBL3945918 156214 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)C(C)(C)NC1=O nan
134147244 156225 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 4 4 6 2.0 CC[C@H](C)[C@@H]1NCCOCCOCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3945984 156225 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 4 4 6 2.0 CC[C@H](C)[C@@H]1NCCOCCOCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134148131 156477 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 568 4 4 6 2.6 COC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3947758 156477 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 568 4 4 6 2.6 COC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
134147387 156596 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 4 4 4 3.9 CC[C@H](C)[C@@H]1NCCCCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3948746 156596 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 518 4 4 4 3.9 CC[C@H](C)[C@@H]1NCCCCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134147861 156636 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 526 2 4 5 2.9 CC1(C)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C(C)(C)NC1=O nan
CHEMBL3949023 156636 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 526 2 4 5 2.9 CC1(C)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C(C)(C)NC1=O nan
134147972 156717 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 488 4 3 5 2.5 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H]([C@H](C)CC)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3949704 156717 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 488 4 3 5 2.5 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H]([C@H](C)CC)NC(=O)[C@@H](C)N(C)C1=O nan
134147412 156745 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.4 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2cccc(C(F)(F)F)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3949926 156745 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.4 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2cccc(C(F)(F)F)c2)NC(=O)C2(CCCC2)NC1=O nan
134148083 156891 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 546 3 4 5 3.4 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCCC2)NC1=O nan
CHEMBL3951110 156891 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 546 3 4 5 3.4 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCCC2)NC1=O nan
134144491 156920 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 504 4 4 4 3.5 CC[C@H](C)[C@@H]1NCCCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3951362 156920 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 504 4 4 4 3.5 CC[C@H](C)[C@@H]1NCCCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134143693 156936 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 4 5 3.1 CC[C@H](C)[C@@H]1NCCOCCCCCNC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3951593 156936 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 4 5 3.1 CC[C@H](C)[C@@H]1NCCOCCCCCNC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134145200 157231 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 550 6 4 6 2.8 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(COCc2ccccc2)NC(=O)C(C)(C)NC1=O nan
CHEMBL3954124 157231 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 550 6 4 6 2.8 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(COCc2ccccc2)NC(=O)C(C)(C)NC1=O nan
134144043 157268 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 570 4 5 6 2.3 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1c[nH]cn1 nan
CHEMBL3954394 157268 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 570 4 5 6 2.3 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1c[nH]cn1 nan
134144941 157306 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.6 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2cc(F)cc(F)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3954620 157306 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.6 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2cc(F)cc(F)c2)NC(=O)C2(CCCC2)NC1=O nan
134144060 157436 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3955632 157436 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134155541 157816 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 4 3.3 CCC(C)C1NCCc2ccccc2CCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3958657 157816 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 4 3.3 CCC(C)C1NCCc2ccccc2CCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
134155247 157829 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 630 4 4 5 4.7 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccc2ccccc2c1 nan
CHEMBL3958739 157829 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 630 4 4 5 4.7 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccc2ccccc2c1 nan
117812381 158130 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 592 3 3 5 3.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(C(F)(F)F)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3961160 158130 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 592 3 3 5 3.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(C(F)(F)F)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134155292 158181 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 458 4 3 5 1.3 CC[C@H](C)[C@@H]1NCCOC/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3961641 158181 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 458 4 3 5 1.3 CC[C@H](C)[C@@H]1NCCOC/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134154704 158189 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 510 2 4 5 3.1 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)C2(CCCC2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3961696 158189 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 510 2 4 5 3.1 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)C2(CCCC2)NC(=O)C2(CCCC2)NC1=O nan
134152627 158327 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 504 4 3 4 3.0 CC[C@H](C)[C@@H]1NCc2ccccc2C/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3963078 158327 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 504 4 3 4 3.0 CC[C@H](C)[C@@H]1NCc2ccccc2C/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134150950 158384 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 5 4 5 2.8 CCC[C@@H]1NC(=O)[C@@H](C(C)C)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3963523 158384 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 5 4 5 2.8 CCC[C@@H]1NC(=O)[C@@H](C(C)C)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC1=O nan
57528212 158602 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 2 2 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN2CCC[C@H]2C(=O)N1C nan
CHEMBL3965338 158602 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 2 2 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN2CCC[C@H]2C(=O)N1C nan
134150767 158605 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 2 4 5 3.0 C[C@@H]1NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
CHEMBL3965351 158605 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 2 4 5 3.0 C[C@@H]1NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
134150369 158635 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 3 5 4.4 CC[C@H](C)[C@@H]1NCCOc2cc(F)ccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)N(C)C1=O nan
CHEMBL3965516 158635 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 3 5 4.4 CC[C@H](C)[C@@H]1NCCOc2cc(F)ccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)N(C)C1=O nan
134150388 158704 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 617 5 4 7 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(NS(C)(=O)=O)cc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3966251 158704 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 617 5 4 7 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(NS(C)(=O)=O)cc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134150696 158858 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 4 3.2 CCC(C)C1NCc2ccccc2CCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3967506 158858 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 4 3.2 CCC(C)C1NCc2ccccc2CCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
134153608 159149 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 4 3.2 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3970180 159149 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 4 3.2 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134154369 159173 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3970414 159173 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134153972 159181 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 526 3 3 6 1.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCOc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3970491 159181 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 526 3 3 6 1.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCOc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134154079 159182 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 512 4 4 5 3.2 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](CC(C)C)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3970499 159182 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 512 4 4 5 3.2 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](CC(C)C)NC(=O)C2(CCCC2)NC1=O nan
134153529 159227 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 548 5 4 5 3.4 CCCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3970856 159227 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 548 5 4 5 3.4 CCCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134154612 159290 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 2 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)N2CC[C@H](C2=O)N(C)C1=O nan
CHEMBL3971356 159290 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 2 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)N2CC[C@H](C2=O)N(C)C1=O nan
134153232 159358 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.5 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@H]1Cc1ccccc1 nan
CHEMBL3971845 159358 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.5 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@H]1Cc1ccccc1 nan
134154534 159523 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 474 3 3 5 1.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCC/C=C\COCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3973254 159523 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 474 3 3 5 1.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCC/C=C\COCCN[C@@H](C2CC2)C(=O)N1C nan
134154022 159604 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3973940 159604 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134151581 159987 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 610 4 4 5 4.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2C(C)(C)CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3977241 159987 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 610 4 4 5 4.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2C(C)(C)CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
57528347 159991 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O nan
CHEMBL3977265 159991 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O nan
134152388 159997 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 594 5 4 5 4.0 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1CCc1ccccc1 nan
CHEMBL3977294 159997 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 594 5 4 5 4.0 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1CCc1ccccc1 nan
134151706 160133 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 3 5 2.4 CC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3978455 160133 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 3 5 2.4 CC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
134151524 160159 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 644 5 4 6 4.2 COc1ccccc1C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3978661 160159 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 644 5 4 6 4.2 COc1ccccc1C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
134152209 160181 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 510 3 4 6 1.0 CC(O)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3978864 160181 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 510 3 4 6 1.0 CC(O)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134152547 160262 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 4 4 5 2.9 CC[C@H](C)[C@@H]1NCCOC/C=C\CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3979606 160262 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 532 4 4 5 2.9 CC[C@H](C)[C@@H]1NCCOC/C=C\CCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
11421086 160345 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 4 2 5 2.8 CCC[C@H]1C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN1C nan
CHEMBL3980276 160345 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 4 2 5 2.8 CCC[C@H]1C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN1C nan
134157913 160410 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 504 3 4 5 2.2 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O nan
CHEMBL3980873 160410 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 504 3 4 5 2.2 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O nan
134156625 160430 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 472 4 3 5 1.7 CC[C@H](C)[C@@H]1NCCOC/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3981072 160430 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 472 4 3 5 1.7 CC[C@H](C)[C@@H]1NCCOC/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134157438 160527 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 505 4 5 5 1.9 CC[C@H](C)[C@@H]1NCCCNCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3981843 160527 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 505 4 5 5 1.9 CC[C@H](C)[C@@H]1NCCCNCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134157625 160540 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.6 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2ccc(F)c(F)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3981960 160540 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 582 4 4 5 3.6 CCC(C)C1NCCOc2ccccc2/C=C\CNC(=O)C(Cc2ccc(F)c(F)c2)NC(=O)C2(CCCC2)NC1=O nan
59834193 160931 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.5 CC1CNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)NCCOc2ccccc2C1 nan
CHEMBL3985477 160931 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.5 CC1CNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)NCCOc2ccccc2C1 nan
134156443 161125 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 550 5 3 5 3.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C(C)C)N(C)C1=O nan
CHEMBL3986906 161125 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 550 5 3 5 3.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C(C)C)N(C)C1=O nan
56926176 75789 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 3 5 2.1 CCC[C@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL1923505 75789 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 3 5 2.1 CCC[C@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
56926266 75791 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 523 6 4 6 1.4 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CCCCN)C1=O nan
CHEMBL1923508 75791 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 523 6 4 6 1.4 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CCCCN)C1=O nan
134133634 150412 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 549 4 4 6 2.7 CC(C)C[C@@H]1NCCOc2cccnc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3899825 150412 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 549 4 4 6 2.7 CC(C)C[C@@H]1NCCOc2cccnc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
57722117 150462 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 466 2 3 5 1.3 C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3900193 150462 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 466 2 3 5 1.3 C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
57722068 150711 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 478 3 3 6 0.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCOCCOCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3902231 150711 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 478 3 3 6 0.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCOCCOCCN[C@@H](C2CC2)C(=O)N1C nan
134135595 150742 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 598 4 4 5 5.1 CC(C)C[C@@H]1NCc2ccccc2Sc2ccccc2CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3902597 150742 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 598 4 4 5 5.1 CC(C)C[C@@H]1NCc2ccccc2Sc2ccccc2CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134139160 152987 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 560 4 3 5 3.7 CC(C)C[C@H]1C(=O)NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN1C nan
CHEMBL3920156 152987 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 560 4 3 5 3.7 CC(C)C[C@H]1C(=O)NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN1C nan
134140250 153024 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 562 5 4 5 3.7 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](CCc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3920479 153024 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 562 5 4 5 3.7 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](CCc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
57951693 153055 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.4 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O nan
CHEMBL3920711 153055 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.4 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O nan
134140177 153148 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CC(C)C[C@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3921493 153148 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CC(C)C[C@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134139639 153417 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 6 4 7 2.5 CCOC(=O)CC[C@@H]1NC(=O)C2(CCCC2)NC(=O)[C@H](CC(C)C)NCCOc2ccccc2/C=C\CNC1=O nan
CHEMBL3923467 153417 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 6 4 7 2.5 CCOC(=O)CC[C@@H]1NC(=O)C2(CCCC2)NC(=O)[C@H](CC(C)C)NCCOc2ccccc2/C=C\CNC1=O nan
134140216 153422 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 587 4 5 5 3.8 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3923508 153422 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 587 4 5 5 3.8 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)C2(CCCC2)NC1=O nan
134141155 153506 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 6 3.3 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCOC2)NC1=O nan
CHEMBL3924187 153506 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 6 3.3 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCOC2)NC1=O nan
134137626 154261 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 4 5 6 3.0 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3930400 154261 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 4 5 6 3.0 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)C2(CCCC2)NC1=O nan
134148332 155060 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 583 4 4 6 3.3 CC[C@H](C)[C@@H]1NCCOc2ncccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3936664 155060 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 583 4 4 6 3.3 CC[C@H](C)[C@@H]1NCCOc2ncccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
57528213 155263 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 3 5 2.9 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O nan
CHEMBL3938163 155263 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 3 5 2.9 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O nan
134149424 155415 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 3 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](C(C)c2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3939431 155415 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 3 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](C(C)c2ccccc2)NC(=O)CN(C)C1=O nan
57951672 156373 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.4 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
CHEMBL3946954 156373 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.4 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
134147008 156715 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 4 4 5 2.8 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C(C)(C)NC1=O nan
CHEMBL3949653 156715 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 4 4 5 2.8 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C(C)(C)NC1=O nan
134155726 157797 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 478 3 3 6 0.2 CC1C(=O)NC(Cc2ccc(F)cc2)C(=O)NCCOCCOCCNC(C2CC2)C(=O)N1C nan
CHEMBL3958492 157797 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 478 3 3 6 0.2 CC1C(=O)NC(Cc2ccc(F)cc2)C(=O)NCCOCCOCCNC(C2CC2)C(=O)N1C nan
134155844 157867 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 570 6 4 5 3.3 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC1=O nan
CHEMBL3959055 157867 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 570 6 4 5 3.3 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC1=O nan
57528307 157906 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O nan
CHEMBL3959346 157906 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O nan
134156186 158129 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 490 4 4 4 3.1 CC[C@H](C)[C@@H]1NCCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3961157 158129 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 490 4 4 4 3.1 CC[C@H](C)[C@@H]1NCCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134150525 158343 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 551 8 5 6 2.2 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O nan
CHEMBL3963236 158343 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 551 8 5 6 2.2 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O nan
134149894 158613 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.2 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccc(Cl)cc1 nan
CHEMBL3965402 158613 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.2 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccc(Cl)cc1 nan
134150119 158826 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 6 4 6 3.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](COC(C)(C)C)NC1=O nan
CHEMBL3967266 158826 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 6 4 6 3.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](COC(C)(C)C)NC1=O nan
134150914 158859 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 6 3 5 3.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]([C@H](C)CC)N(C)C1=O nan
CHEMBL3967522 158859 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 6 3 5 3.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]([C@H](C)CC)N(C)C1=O nan
57722047 159646 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 436 4 3 4 1.8 CCC[C@@H]1NCc2cccc(c2)CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3974323 159646 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 436 4 3 4 1.8 CCC[C@@H]1NCc2cccc(c2)CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
57951687 159651 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 4 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O nan
CHEMBL3974356 159651 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 4 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O nan
57528291 159695 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 3 5 2.9 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O nan
CHEMBL3974776 159695 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 3 5 2.9 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O nan
134152485 159955 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 604 5 4 6 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(C(=O)O)cc2)NC(=O)C2(CCCC2)N(C)C1=O nan
CHEMBL3976941 159955 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 604 5 4 6 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(C(=O)O)cc2)NC(=O)C2(CCCC2)N(C)C1=O nan
134151873 159979 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 630 4 4 5 4.7 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1cccc2ccccc12 nan
CHEMBL3977166 159979 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 630 4 4 5 4.7 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1cccc2ccccc12 nan
76556607 160334 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 2 5 2.8 CCC(C)C1NCCOc2ccccc2CCCNC(=O)C(Cc2ccccc2)N2CCC(C2=O)N(C)C1=O nan
CHEMBL3980176 160334 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 2 5 2.8 CCC(C)C1NCCOc2ccccc2CCCNC(=O)C(Cc2ccccc2)N2CCC(C2=O)N(C)C1=O nan
134157812 160449 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 4 5 2.1 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O nan
CHEMBL3981235 160449 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 4 5 2.1 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O nan
134156737 160478 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 547 4 4 6 2.8 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccncc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3981446 160478 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 547 4 4 6 2.8 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccncc2)NC(=O)C2(CCCC2)NC1=O nan
134156806 160873 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 6 4 5 3.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(C)C)NC1=O nan
CHEMBL3984892 160873 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 6 4 5 3.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(C)C)NC1=O nan
134157124 160985 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 492 2 4 5 1.9 O=C1CNCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)N1 nan
CHEMBL3985913 160985 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 492 2 4 5 1.9 O=C1CNCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)N1 nan
11706547 75821 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 540 3 3 5 2.8 CC(C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923619 75821 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 540 3 3 5 2.8 CC(C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
134138625 154809 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 3 3 5 1.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3934561 154809 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 3 3 5 1.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
44434011 154642 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 465 12 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL393321 154642 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 465 12 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCc1ccccc1 10.1016/j.bmcl.2007.07.099
70692601 82650 0 None - 1 Human 8.0 pKi = 8.0 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 481 7 0 7 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048814 82650 0 None - 1 Human 8.0 pKi = 8.0 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 481 7 0 7 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
127046957 146485 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 649 12 3 7 5.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc(F)cc(F)n2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798155 146485 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 649 12 3 7 5.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc(F)cc(F)n2)cc1 10.1016/j.bmcl.2016.04.003
127046472 146472 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798056 146472 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
56926266 75791 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 523 6 4 6 1.4 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CCCCN)C1=O 10.1021/jm2007062
CHEMBL1923508 75791 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 523 6 4 6 1.4 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CCCCN)C1=O 10.1021/jm2007062
73352329 99040 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 6 0 6 3.8 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H](C)c2ccc(-c4ncccn4)cc2)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426669 99040 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 6 0 6 3.8 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H](C)c2ccc(-c4ncccn4)cc2)C3)nc1 10.1016/j.bmcl.2013.07.044
70692602 82651 0 None - 1 Human 6.9 pKi = 6.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 423 8 0 5 3.5 CCCOc1ccc(CN2CC3(CCN(C(=O)Cc4ccc(OC)cc4)CC3)C2)cn1 10.1016/j.bmcl.2012.05.024
CHEMBL2048815 82651 0 None - 1 Human 6.9 pKi = 6.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 423 8 0 5 3.5 CCCOc1ccc(CN2CC3(CCN(C(=O)Cc4ccc(OC)cc4)CC3)C2)cn1 10.1016/j.bmcl.2012.05.024
162665974 189014 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 612 13 3 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4783347 189014 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 612 13 3 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
44396381 74305 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 558 13 2 3 6.2 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NCc1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm040103i
CHEMBL189625 74305 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 558 13 2 3 6.2 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NCc1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm040103i
44396377 73717 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 532 13 2 4 5.8 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(Cc1ccc(C)o1)C(=O)NC1CCCCC1 10.1021/jm040103i
CHEMBL186647 73717 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 532 13 2 4 5.8 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(Cc1ccc(C)o1)C(=O)NC1CCCCC1 10.1021/jm040103i
44396269 74130 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 426 10 2 3 4.2 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C)C(=O)NC(C)(C)C 10.1021/jm040103i
CHEMBL188586 74130 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 426 10 2 3 4.2 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C)C(=O)NC(C)(C)C 10.1021/jm040103i
56926895 75840 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 552 3 3 5 3.0 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OC(C)(C)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923639 75840 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 552 3 3 5 3.0 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OC(C)(C)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
56942244 131975 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645259 131975 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
162648546 186657 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 536 13 3 6 3.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC=O)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4745666 186657 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 536 13 3 6 3.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC=O)cc1 10.1021/acs.jmedchem.9b02122
58438460 118515 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL3287217 118515 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml400473x
56926356 75794 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923512 75794 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
56926176 75789 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 3 5 2.1 CCC[C@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923505 75789 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 3 5 2.1 CCC[C@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
71453390 88618 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 526 6 2 4 4.4 C=CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164500 88618 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 526 6 2 4 4.4 C=CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
162663952 188931 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 636 13 2 7 6.6 COc1ccc(/C=C(\C#N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4782383 188931 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 636 13 2 7 6.6 COc1ccc(/C=C(\C#N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
118725963 123972 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 541 7 1 7 3.6 COc1ccc(OCC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
CHEMBL3394203 123972 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 541 7 1 7 3.6 COc1ccc(OCC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
44434112 175639 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2cc3ccccc3n2S(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL438154 175639 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2cc3ccccc3n2S(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
3174463 73542 4 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 532 12 2 3 6.2 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(F)cc1 10.1021/jm040103i
CHEMBL185876 73542 4 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 532 12 2 3 6.2 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(F)cc1 10.1021/jm040103i
56926464 75814 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)N(C)C1=O nan
CHEMBL1923612 75814 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)N(C)C1=O nan
118725960 123968 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 507 5 0 6 4.5 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C#N)c1 10.1021/ml500414n
CHEMBL3394199 123968 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 507 5 0 6 4.5 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C#N)c1 10.1021/ml500414n
162657547 187762 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 694 15 2 9 6.2 COc1ccc(/C=C(\C#N)C(=O)OCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4758721 187762 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 694 15 2 9 6.2 COc1ccc(/C=C(\C#N)C(=O)OCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
162658148 187927 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 565 13 4 7 3.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CN)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4760746 187927 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 565 13 4 7 3.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CN)cc1 10.1021/acs.jmedchem.9b02122
162662164 188189 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 636 12 3 6 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C#Cc2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4763700 188189 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 636 12 3 6 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C#Cc2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
127047362 146497 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 590 11 5 7 4.7 COc1ccc(Cn2c([C@H](N)Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798204 146497 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 590 11 5 7 4.7 COc1ccc(Cn2c([C@H](N)Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
3154000 131048 4 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 530 12 3 4 5.8 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(O)cc1 10.1021/jm040103i
CHEMBL363467 131048 4 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 530 12 3 4 5.8 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(O)cc1 10.1021/jm040103i
162651277 186975 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 598 14 3 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNCc2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4749525 186975 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 598 14 3 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNCc2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
3180629 74127 5 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 518 11 2 3 5.8 CCN(CC)CCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(F)cc1 10.1021/jm040103i
CHEMBL188582 74127 5 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 518 11 2 3 5.8 CCN(CC)CCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(F)cc1 10.1021/jm040103i
44434016 96968 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 415 12 3 7 1.5 CCCCNC(=O)CCn1nnnc1[C@@H](CCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL238228 96968 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 415 12 3 7 1.5 CCCCNC(=O)CCn1nnnc1[C@@H](CCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
72190452 99053 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 474 5 0 6 4.4 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H]2CCc4cc(-c5nccs5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426682 99053 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 474 5 0 6 4.4 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H]2CCc4cc(-c5nccs5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
118725964 123973 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 539 7 1 6 4.1 COc1ccc(CCC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
CHEMBL3394204 123973 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 539 7 1 6 4.1 COc1ccc(CCC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
70692600 82649 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 447 7 0 7 2.8 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048813 82649 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 447 7 0 7 2.8 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
70682036 82653 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 446 7 1 4 4.3 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4n[nH]c5ccccc45)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048817 82653 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 446 7 1 4 4.3 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4n[nH]c5ccccc45)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
70686293 82658 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 472 5 0 7 3.8 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-c5ncccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048822 82658 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 472 5 0 7 3.8 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-c5ncccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
58438460 118515 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml500414n
CHEMBL3287217 118515 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml500414n
162660604 187998 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 700 15 3 9 5.0 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCN3CCCCC3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4761319 187998 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 700 15 3 9 5.0 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCN3CCCCC3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
162671996 189610 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 707 16 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)NCCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4791255 189610 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 707 16 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)NCCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
25032438 122974 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human ghrelin receptor by receptor binding assayBinding affinity to human ghrelin receptor by receptor binding assay
ChEMBL 485 14 2 6 3.8 CCN(CC)CCCS(=O)(=O)N[C@H](CCc1ccccc1)c1nc(-c2ccc(OC)cc2)n[nH]1 10.1021/jm5003183
CHEMBL3358450 122974 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human ghrelin receptor by receptor binding assayBinding affinity to human ghrelin receptor by receptor binding assay
ChEMBL 485 14 2 6 3.8 CCN(CC)CCCS(=O)(=O)N[C@H](CCc1ccccc1)c1nc(-c2ccc(OC)cc2)n[nH]1 10.1021/jm5003183
11692516 75823 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 554 3 3 5 3.1 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923621 75823 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 554 3 3 5 3.1 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
67407161 99059 0 None 1819 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 467 5 0 5 4.3 CCc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426688 99059 0 None 1819 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 467 5 0 5 4.3 CCc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
67410074 118514 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccc(C)n5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL3287216 118514 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccc(C)n5)ccc42)C3)nc1 10.1021/ml400473x
56926782 75832 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 472 4 3 4 3.0 CC[C@H](C)[C@@H]1NCCCCCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923631 75832 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 472 4 3 4 3.0 CC[C@H](C)[C@@H]1NCCCCCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
70696687 82648 0 None - 1 Human 6.8 pKi = 6.8 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 446 7 0 6 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4cccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048812 82648 0 None - 1 Human 6.8 pKi = 6.8 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 446 7 0 6 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4cccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
127046806 146711 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 638 13 4 7 5.4 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799604 146711 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 638 13 4 7 5.4 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
127048038 146750 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 551 11 4 7 4.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799862 146750 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 551 11 4 7 4.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
44434076 96552 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 513 10 2 9 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC1CN(S(C)(=O)=O)c2ccccc21 10.1016/j.bmcl.2007.07.099
CHEMBL237717 96552 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 513 10 2 9 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC1CN(S(C)(=O)=O)c2ccccc21 10.1016/j.bmcl.2007.07.099
56926463 75813 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923611 75813 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
11526696 78377 17 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923502 78377 17 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1963249 78377 17 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
72191051 99037 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 456 5 0 6 3.4 CCc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426666 99037 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 456 5 0 6 3.4 CCc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
58438460 118515 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL3287217 118515 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml400473x
56926783 75833 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 470 4 3 4 2.8 CC[C@H](C)[C@@H]1NCCCC/C=C/CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923632 75833 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 470 4 3 4 2.8 CC[C@H](C)[C@@H]1NCCCC/C=C/CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
162658631 187862 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 561 12 3 7 3.6 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C#N)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4759983 187862 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 561 12 3 7 3.6 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C#N)cc1 10.1021/acs.jmedchem.9b02122
118725958 123967 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 507 4 0 7 3.9 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)Cc4nn(C)c5ncccc45)CC3)C2)ncn1 10.1021/ml500414n
CHEMBL3394197 123967 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 507 4 0 7 3.9 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)Cc4nn(C)c5ncccc45)CC3)C2)ncn1 10.1021/ml500414n
162659337 188095 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 665 15 3 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C(C#N)Cc2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4762631 188095 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 665 15 3 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C(C#N)Cc2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
73355325 99042 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 6 0 6 3.8 COc1ccc(CC(=O)N2CCC3(CC2)CN(C(C)c2ccc(-c4ncccn4)cc2)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426671 99042 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 6 0 6 3.8 COc1ccc(CC(=O)N2CCC3(CC2)CN(C(C)c2ccc(-c4ncccn4)cc2)C3)nc1 10.1016/j.bmcl.2013.07.044
70696688 82654 0 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 487 9 0 6 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cn1 10.1016/j.bmcl.2012.05.024
CHEMBL2048818 82654 0 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 487 9 0 6 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cn1 10.1016/j.bmcl.2012.05.024
127048060 146639 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 789 20 6 10 5.4 COC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799222 146639 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 789 20 6 10 5.4 COC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
56942388 146721 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799687 146721 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
162677361 190288 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 685 16 4 8 4.7 COc1ccc(C[C@@H](N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4799766 190288 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 685 16 4 8 4.7 COc1ccc(C[C@@H](N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
58438475 99048 0 None 1548 2 Human 7.8 pKi = 7.8 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml400473x
CHEMBL2426677 99048 0 None 1548 2 Human 7.8 pKi = 7.8 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml400473x
44434109 153059 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 529 13 2 9 1.8 CN(c1ccccc1CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N)S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL392076 153059 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 529 13 2 9 1.8 CN(c1ccccc1CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N)S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
134139080 154461 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
CHEMBL3931856 154461 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
44434010 95548 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 445 14 3 8 1.5 CCCCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL236311 95548 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 445 14 3 8 1.5 CCCCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
127047655 146392 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797531 146392 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
44340007 16086 0 None - 1 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 541 9 2 6 2.0 CN1N=C2CCN(C(=O)[C@@H](COCc3ccc(F)c(F)c3)NC(=O)C(C)(C)N)CC2(Cc2ccccc2)C1=O 10.1016/s0960-894x(02)00734-5
CHEMBL111026 16086 0 None - 1 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 541 9 2 6 2.0 CN1N=C2CCN(C(=O)[C@@H](COCc3ccc(F)c(F)c3)NC(=O)C(C)(C)N)CC2(Cc2ccccc2)C1=O 10.1016/s0960-894x(02)00734-5
56925344 75842 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 550 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cccc3c2O[C@@H](CC3)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923641 75842 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 550 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cccc3c2O[C@@H](CC3)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
44434083 96806 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 420 10 2 7 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C/C=C/c1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL238155 96806 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 420 10 2 7 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C/C=C/c1ccccc1 10.1016/j.bmcl.2007.07.099
44434050 152228 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL391428 152228 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1 10.1016/j.bmcl.2007.07.099
44396306 74051 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 452 11 2 3 4.7 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C)C(=O)NC1CCCCC1 10.1021/jm040103i
CHEMBL188173 74051 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 452 11 2 3 4.7 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C)C(=O)NC1CCCCC1 10.1021/jm040103i
145948725 174276 0 None - 1 Human 8.7 pKi = 8.7 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 885 20 7 9 6.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL4299615 174276 0 None - 1 Human 8.7 pKi = 8.7 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 885 20 7 9 6.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
57345597 78045 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 410 5 0 6 4.2 Cc1nc2ccc(Oc3ccc(F)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956988 78045 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 410 5 0 6 4.2 Cc1nc2ccc(Oc3ccc(F)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
56942243 131974 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645258 131974 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 10.1016/j.bmcl.2016.04.003
162648837 186617 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 706 15 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4745116 186617 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 706 15 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
127048059 146344 0 None - 1 Human 8.6 pKi = 8.6 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 675 16 6 8 4.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797225 146344 0 None - 1 Human 8.6 pKi = 8.6 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 675 16 6 8 4.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
11526745 75843 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923642 75843 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
57400003 78054 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 461 5 0 7 4.7 Cc1nc2ccc(Oc3ccc(F)c4cccnc34)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956996 78054 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 461 5 0 7 4.7 Cc1nc2ccc(Oc3ccc(F)c4cccnc34)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
155529391 178219 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1427 41 20 17 -3.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4463042 178219 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1427 41 20 17 -3.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
70690449 82646 0 None - 1 Human 7.7 pKi = 7.7 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 486 9 0 5 4.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048810 82646 0 None - 1 Human 7.7 pKi = 7.7 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 486 9 0 5 4.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
118725965 123974 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 539 6 1 6 4.0 CNC(=O)c1cc(OC)ccc1CC(=O)N1CCC2(CC1)CN([C@@H]1CCc3cc(-c4cc(C)ncn4)ccc31)C2 10.1021/ml500414n
CHEMBL3394205 123974 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 539 6 1 6 4.0 CNC(=O)c1cc(OC)ccc1CC(=O)N1CCC2(CC1)CN([C@@H]1CCc3cc(-c4cc(C)ncn4)ccc31)C2 10.1021/ml500414n
44434080 96686 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL237933 96686 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2007.07.099
162647450 186650 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 536 12 2 6 4.6 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN(C)C)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4745548 186650 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 536 12 2 6 4.6 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN(C)C)cc1 10.1021/acs.jmedchem.9b02122
71456910 88676 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 480 5 2 4 3.6 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164823 88676 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 480 5 2 4 3.6 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
3154005 73547 5 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 550 13 1 4 5.7 CCN(CC)CCCN(C(=O)CCN1CCCc2ccccc21)C(C(=O)NC1CCCCC1)c1ccc(F)cc1 10.1021/jm040103i
CHEMBL185887 73547 5 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 550 13 1 4 5.7 CCN(CC)CCCN(C(=O)CCN1CCCc2ccccc21)C(C(=O)NC1CCCCC1)c1ccc(F)cc1 10.1021/jm040103i
70696689 82657 0 None - 1 Human 6.7 pKi = 6.7 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 460 5 0 7 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5cccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048821 82657 0 None - 1 Human 6.7 pKi = 6.7 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 460 5 0 7 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5cccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
56926681 75826 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2cccc(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923624 75826 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2cccc(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
127047409 146409 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 888 24 8 10 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C(CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797639 146409 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 888 24 8 10 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C(CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
56926785 75835 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923634 75835 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
70688404 82642 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1021/ml400473x
CHEMBL2048807 82642 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1021/ml400473x
44434009 174232 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 431 13 3 8 1.1 CCCCNC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL429799 174232 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 431 13 3 8 1.1 CCCCNC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
53248756 67955 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I]Ghrelin binding to human Ghrelin receptor expressed in CHO-K1 cells after 60 mins by liquid scintillation spectrometryInhibition of [125I]Ghrelin binding to human Ghrelin receptor expressed in CHO-K1 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 457 5 0 5 5.6 Cc1ccccc1-c1nc2ccc(Oc3ccc(F)cc3)cc2c(=O)n1C[C@H]1CCCN(C)C1 10.1016/j.bmc.2011.02.021
CHEMBL1765654 67955 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I]Ghrelin binding to human Ghrelin receptor expressed in CHO-K1 cells after 60 mins by liquid scintillation spectrometryInhibition of [125I]Ghrelin binding to human Ghrelin receptor expressed in CHO-K1 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 457 5 0 5 5.6 Cc1ccccc1-c1nc2ccc(Oc3ccc(F)cc3)cc2c(=O)n1C[C@H]1CCCN(C)C1 10.1016/j.bmc.2011.02.021
CHEMBL2170701 216140 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cn(C)c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
10253999 130571 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 466 12 2 3 5.1 CCC(C(=O)NC1CCCCC1)N(CCCN(CC)CC)C(=O)c1ccc(-c2ccccc2)[nH]1 10.1021/jm040103i
CHEMBL362303 130571 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 466 12 2 3 5.1 CCC(C(=O)NC1CCCCC1)N(CCCN(CC)CC)C(=O)c1ccc(-c2ccccc2)[nH]1 10.1021/jm040103i
127048061 146514 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 903 24 7 11 5.9 COC(=O)[C@H](CC(C)C)NC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798337 146514 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 903 24 7 11 5.9 COC(=O)[C@H](CC(C)C)NC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
162662593 188749 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 591 12 3 7 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN2CCC(N)CC2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4780100 188749 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 591 12 3 7 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN2CCC(N)CC2)cc1 10.1021/acs.jmedchem.9b02122
44579909 193682 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL489819 193682 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
44434073 96375 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL237507 96375 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
70694649 82659 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 475 5 0 7 3.2 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-n3nccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
CHEMBL2048823 82659 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 475 5 0 7 3.2 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-n3nccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
162659161 188170 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 642 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)Cc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4763471 188170 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 642 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)Cc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
162652815 187155 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 564 14 2 6 5.3 CCN(CC)CC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4751674 187155 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 564 14 2 6 5.3 CCN(CC)CC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL2170779 216145 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44434008 153312 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 404 11 2 9 0.7 COC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL392268 153312 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 404 11 2 9 0.7 COC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
44434110 95287 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 515 13 3 9 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL235135 95287 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 515 13 3 9 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
44577060 194831 0 None -69 8 Human 6.6 pKi = 6.6 Binding
Inhibition of ghrelin receptorInhibition of ghrelin receptor
ChEMBL 530 10 1 4 4.8 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL497746 194831 0 None -69 8 Human 6.6 pKi = 6.6 Binding
Inhibition of ghrelin receptorInhibition of ghrelin receptor
ChEMBL 530 10 1 4 4.8 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL2170780 216146 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
71453404 88678 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)N[C@]2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164826 88678 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)N[C@]2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
70692603 82652 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 463 7 0 5 5.0 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4nc5ccccc5s4)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048816 82652 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 463 7 0 5 5.0 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4nc5ccccc5s4)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
56926360 75810 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 522 4 3 5 2.7 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923608 75810 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 522 4 3 5 2.7 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
72190451 99051 0 None 524 2 Human 7.6 pKi = 7.6 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL2426680 99051 0 None 524 2 Human 7.6 pKi = 7.6 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1021/ml400473x
44579907 193827 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)[C@H](C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL491044 193827 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)[C@H](C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
73350846 99041 0 None -1 2 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 6 0 6 3.8 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H](C)c2ccc(-c4ncccn4)cc2)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426670 99041 0 None -1 2 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 6 0 6 3.8 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H](C)c2ccc(-c4ncccn4)cc2)C3)nc1 10.1016/j.bmcl.2013.07.044
44576247 221001 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity at GHS-R1a (unknown origin) assessed as inhibition constantBinding affinity at GHS-R1a (unknown origin) assessed as inhibition constant
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.1c02191
CHEMBL506986 221001 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity at GHS-R1a (unknown origin) assessed as inhibition constantBinding affinity at GHS-R1a (unknown origin) assessed as inhibition constant
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.1c02191
44576247 221001 0 None - 1 Human 6.6 pKi = 6.6 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1016/j.bmcl.2016.04.003
CHEMBL506986 221001 0 None - 1 Human 6.6 pKi = 6.6 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1016/j.bmcl.2016.04.003
44579880 193614 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL489401 193614 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
118725962 123971 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 526 6 1 7 3.1 COc1cc(C(N)=O)c(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccc(C)n5)ccc42)C3)cn1 10.1021/ml500414n
CHEMBL3394202 123971 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 526 6 1 7 3.1 COc1cc(C(N)=O)c(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccc(C)n5)ccc42)C3)cn1 10.1021/ml500414n
44396384 74182 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 574 14 2 5 6.1 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(OC)c(OC)c1 10.1021/jm040103i
CHEMBL188839 74182 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 574 14 2 5 6.1 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(OC)c(OC)c1 10.1021/jm040103i
44434074 161452 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL399625 161452 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
70684155 82660 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 486 5 0 6 4.1 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-c3ncccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
CHEMBL2048824 82660 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 486 5 0 6 4.1 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-c3ncccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
72191050 99038 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 453 4 0 5 4.0 Cc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426667 99038 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 453 4 0 5 4.0 Cc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
72190449 99047 0 None 4 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426676 99047 0 None 4 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
118725966 123975 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 539 6 1 6 4.6 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(NC(C)=O)c1 10.1021/ml500414n
CHEMBL3394206 123975 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 539 6 1 6 4.6 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(NC(C)=O)c1 10.1021/ml500414n
162675268 190137 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 645 13 3 8 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C2(C#N)CCOCC2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4797685 190137 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 645 13 3 8 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C2(C#N)CCOCC2)cc1 10.1021/acs.jmedchem.9b02122
3153999 133609 3 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 494 14 2 3 5.9 CCCCC(C(=O)NC1CCCCC1)N(CCCN(CC)CC)C(=O)c1ccc(-c2ccccc2)[nH]1 10.1021/jm040103i
CHEMBL365489 133609 3 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 494 14 2 3 5.9 CCCCC(C(=O)NC1CCCCC1)N(CCCN(CC)CC)C(=O)c1ccc(-c2ccccc2)[nH]1 10.1021/jm040103i
71451551 88626 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 460 5 2 4 3.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(C)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164508 88626 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 460 5 2 4 3.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(C)cc32)CC1 10.1016/j.bmc.2012.07.018
72190451 99051 0 None 524 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426680 99051 0 None 524 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
72190451 99051 0 None 524 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL2426680 99051 0 None 524 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1021/ml400473x
9950632 95481 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2007.07.099
CHEMBL236038 95481 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2007.07.099
127046472 146472 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at GHS-R1a (unknown origin) assessed as inhibition constantBinding affinity at GHS-R1a (unknown origin) assessed as inhibition constant
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1021/acs.jmedchem.1c02191
CHEMBL3798056 146472 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at GHS-R1a (unknown origin) assessed as inhibition constantBinding affinity at GHS-R1a (unknown origin) assessed as inhibition constant
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1021/acs.jmedchem.1c02191
127045859 146477 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at GHS-R1a (unknown origin) assessed as inhibition constantBinding affinity at GHS-R1a (unknown origin) assessed as inhibition constant
ChEMBL 831 20 7 9 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CO)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1021/acs.jmedchem.1c02191
CHEMBL3798095 146477 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at GHS-R1a (unknown origin) assessed as inhibition constantBinding affinity at GHS-R1a (unknown origin) assessed as inhibition constant
ChEMBL 831 20 7 9 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CO)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1021/acs.jmedchem.1c02191
127045859 146477 0 None - 1 Human 8.5 pKi = 8.5 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 831 20 7 9 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CO)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798095 146477 0 None - 1 Human 8.5 pKi = 8.5 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 831 20 7 9 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CO)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
127047523 146841 0 None - 1 Human 8.5 pKi = 8.5 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 859 20 7 9 6.0 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3800422 146841 0 None - 1 Human 8.5 pKi = 8.5 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 859 20 7 9 6.0 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)O)cc1 10.1016/j.bmcl.2016.04.003
71456897 88625 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 513 5 2 3 5.7 CCN1CCC(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164507 88625 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 513 5 2 3 5.7 CCN1CCC(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
162653916 187324 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 707 15 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4753794 187324 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 707 15 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
162643920 188559 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 679 14 4 8 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4777792 188559 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 679 14 4 8 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
155537651 179095 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1597 47 22 19 -3.8 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(N)=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4475293 179095 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1597 47 22 19 -3.8 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(N)=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
57391292 78053 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 473 6 0 8 4.6 COc1ccc2cccc(Oc3ccc4nc(C)n(C[C@H]5CCCN(C(C)C)C5)c(=O)c4n3)c2n1 10.1016/j.bmcl.2012.01.078
CHEMBL1956995 78053 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 473 6 0 8 4.6 COc1ccc2cccc(Oc3ccc4nc(C)n(C[C@H]5CCCN(C(C)C)C5)c(=O)c4n3)c2n1 10.1016/j.bmcl.2012.01.078
57345598 78062 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 411 5 0 7 3.5 Cc1nc2ncc(Oc3ccc(F)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957004 78062 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 411 5 0 7 3.5 Cc1nc2ncc(Oc3ccc(F)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
53373577 99057 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 458 5 0 7 2.8 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426686 99057 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 458 5 0 7 2.8 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
57391294 78056 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 410 5 0 6 4.2 Cc1nc2cnc(Oc3ccc(F)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956998 78056 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 410 5 0 6 4.2 Cc1nc2cnc(Oc3ccc(F)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
155526063 177815 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1174 34 16 14 -2.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4456830 177815 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1174 34 16 14 -2.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
162663004 188828 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 603 13 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C(C)(C)C#N)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4781141 188828 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 603 13 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C(C)(C)C#N)cc1 10.1021/acs.jmedchem.9b02122
155557019 181366 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4556887 181366 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
71453489 216147 15 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.8b01644
CHEMBL2170781 216147 15 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.8b01644
67405379 99054 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 474 5 0 6 4.4 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccs5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426683 99054 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 474 5 0 6 4.4 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccs5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
25211977 193681 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 372 7 1 3 3.9 C[C@H](Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL489818 193681 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 372 7 1 3 3.9 C[C@H](Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
25098836 198237 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL519322 198237 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
127047525 146545 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 858 20 7 9 5.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798559 146545 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 858 20 7 9 5.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
162653309 187252 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 718 14 5 8 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4752936 187252 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 718 14 5 8 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
44579756 193602 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL489370 193602 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
162666964 189289 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 536 13 3 6 4.6 CCNCC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4787023 189289 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 536 13 3 6 4.6 CCNCC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL2170693 216132 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1csc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44434121 96683 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 385 11 2 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCC#N 10.1016/j.bmcl.2007.07.099
CHEMBL237927 96683 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 385 11 2 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCC#N 10.1016/j.bmcl.2007.07.099
56926584 75822 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 554 4 3 5 3.2 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923620 75822 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 554 4 3 5 3.2 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
44434120 96682 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 523 15 3 9 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCCNC(=O)OCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL237926 96682 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 523 15 3 9 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCCNC(=O)OCc1ccccc1 10.1016/j.bmcl.2007.07.099
44434007 95350 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 390 10 2 9 0.3 COC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL235446 95350 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 390 10 2 9 0.3 COC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
11541143 75820 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 540 4 3 5 3.0 CCC[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923618 75820 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 540 4 3 5 3.0 CCC[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
24969520 75824 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 520 3 3 5 2.5 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923622 75824 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 520 3 3 5 2.5 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL2170694 216133 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
56926580 75816 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 536 5 4 5 3.1 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CC)NC1=O 10.1021/jm2007062
CHEMBL1923614 75816 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 536 5 4 5 3.1 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CC)NC1=O 10.1021/jm2007062
162653802 187310 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 656 15 4 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CCc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4753592 187310 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 656 15 4 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CCc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
73346226 99039 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 487 8 0 7 3.4 COCC(c1ccc(-c2ncccn2)cc1)N1CC2(CCN(C(=O)Cc3ccc(OC)cn3)CC2)C1 10.1016/j.bmcl.2013.07.044
CHEMBL2426668 99039 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 487 8 0 7 3.4 COCC(c1ccc(-c2ncccn2)cc1)N1CC2(CCN(C(=O)Cc3ccc(OC)cn3)CC2)C1 10.1016/j.bmcl.2013.07.044
162674738 190166 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 638 14 3 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4797988 190166 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 638 14 3 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
56926177 75790 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923506 75790 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
56926581 75817 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 550 5 4 5 3.4 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C(C)C)NC1=O 10.1021/jm2007062
CHEMBL1923615 75817 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 550 5 4 5 3.4 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C(C)C)NC1=O 10.1021/jm2007062
71458747 88613 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2012.07.018
CHEMBL2164494 88613 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2012.07.018
23631116 10884 23 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 409 5 0 5 4.8 Fc1ccc(cc1)Oc1ccc2c(c1)c(=O)n(c(n2)C)C[C@H]1CCCN(C1)C(C)C 10.1016/j.bmcl.2012.01.078
3538 10884 23 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 409 5 0 5 4.8 Fc1ccc(cc1)Oc1ccc2c(c1)c(=O)n(c(n2)C)C[C@H]1CCCN(C1)C(C)C 10.1016/j.bmcl.2012.01.078
CHEMBL243001 10884 23 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 409 5 0 5 4.8 Fc1ccc(cc1)Oc1ccc2c(c1)c(=O)n(c(n2)C)C[C@H]1CCCN(C1)C(C)C 10.1016/j.bmcl.2012.01.078
127046956 146735 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 631 12 3 7 5.5 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799776 146735 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 631 12 3 7 5.5 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2016.04.003
118725961 123969 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 523 6 0 7 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C#N)c1 10.1021/ml500414n
CHEMBL3394200 123969 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 523 6 0 7 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C#N)c1 10.1021/ml500414n
162663407 188809 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 562 13 3 6 4.3 C=CC(=O)NCC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4780843 188809 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 562 13 3 6 4.3 C=CC(=O)NCC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
56926462 75812 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923610 75812 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
70695747 79966 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Ghrelin from human GHSR1a receptorDisplacement of [125I]Ghrelin from human GHSR1a receptor
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011816 79966 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Ghrelin from human GHSR1a receptorDisplacement of [125I]Ghrelin from human GHSR1a receptor
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
67406334 118511 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 498 4 0 7 4.3 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN([C@@H]3CCc5cc(-c6ncccn6)ccc53)C4)nc2s1 10.1021/ml400473x
CHEMBL3287213 118511 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 498 4 0 7 4.3 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN([C@@H]3CCc5cc(-c6ncccn6)ccc53)C4)nc2s1 10.1021/ml400473x
57390496 75830 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
CHEMBL1923628 75830 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
71453489 216147 15 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 216147 15 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
56926269 75793 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 460 5 3 5 2.0 CCCC[C@H]1NC(=O)CN(C)C(=O)[C@H](CCC)NCCOc2ccccc2CCCNC1=O 10.1021/jm2007062
CHEMBL1923511 75793 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 460 5 3 5 2.0 CCCC[C@H]1NC(=O)CN(C)C(=O)[C@H](CCC)NCCOc2ccccc2CCCNC1=O 10.1021/jm2007062
56926784 75834 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 506 4 3 4 2.9 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923633 75834 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 506 4 3 4 2.9 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
70688404 82642 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1021/ml400473x
CHEMBL2048807 82642 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1021/ml400473x
70688404 82642 0 None - 1 Human 6.4 pKi = 6.4 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048807 82642 0 None - 1 Human 6.4 pKi = 6.4 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1016/j.bmcl.2012.05.024
44434123 152328 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 343 8 2 8 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC#N 10.1016/j.bmcl.2007.07.099
CHEMBL391510 152328 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 343 8 2 8 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC#N 10.1016/j.bmcl.2007.07.099
56926582 75818 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](CCc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923616 75818 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](CCc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
16114404 161676 24 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 508 11 3 6 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL400814 161676 24 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 508 11 3 6 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/acs.jmedchem.9b02122
25190383 88684 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164831 88684 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
11683187 206711 44 None -457 5 Human 5.4 pKi = 5.4 Binding
Binding affinity to ghrelin receptorBinding affinity to ghrelin receptor
ChEMBL 419 7 0 8 2.9 COCc1nnc(N2CC(Oc3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1016/j.bmcl.2009.11.097
CHEMBL594828 206711 44 None -457 5 Human 5.4 pKi = 5.4 Binding
Binding affinity to ghrelin receptorBinding affinity to ghrelin receptor
ChEMBL 419 7 0 8 2.9 COCc1nnc(N2CC(Oc3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1016/j.bmcl.2009.11.097
70684154 82644 0 None - 1 Human 6.4 pKi = 6.4 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 414 6 0 4 3.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccccc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048809 82644 0 None - 1 Human 6.4 pKi = 6.4 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 414 6 0 4 3.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccccc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
44434055 96080 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL236858 96080 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
56942385 131976 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645260 131976 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
56942535 146539 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 593 12 4 7 4.4 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798525 146539 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 593 12 4 7 4.4 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
24180592 103788 0 None -134 6 Human 6.3 pKi = 6.3 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
CHEMBL266647 103788 0 None -134 6 Human 6.3 pKi = 6.3 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
44434113 95424 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 452 10 2 9 1.5 COC(=O)C(c1ccccc1)n1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL235793 95424 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 452 10 2 9 1.5 COC(=O)C(c1ccccc1)n1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
44434051 96190 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccccc2)n1 10.1016/j.bmcl.2007.07.099
CHEMBL237058 96190 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccccc2)n1 10.1016/j.bmcl.2007.07.099
118725954 123965 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 467 4 0 5 4.3 Cc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml500414n
CHEMBL3394193 123965 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 467 4 0 5 4.3 Cc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml500414n
24969603 75829 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 520 3 3 5 2.4 Cc1ccc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NCCOc3ccccc3CCCNC2=O)cc1 10.1021/jm2007062
CHEMBL1923627 75829 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 520 3 3 5 2.4 Cc1ccc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NCCOc3ccccc3CCCNC2=O)cc1 10.1021/jm2007062
57394882 78069 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 447 5 0 9 3.3 Cc1nc2ncc(Oc3ccc4c(c3)ncn4C)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957011 78069 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 447 5 0 9 3.3 Cc1nc2ncc(Oc3ccc4c(c3)ncn4C)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
9876514 15912 2 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 610 10 2 7 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)cc1F)C(=O)N1CCC2=NN(CC(F)(F)F)C(=O)[C@]2(Cc2ccccn2)C1 10.1016/s0960-894x(02)00734-5
CHEMBL109980 15912 2 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 610 10 2 7 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)cc1F)C(=O)N1CCC2=NN(CC(F)(F)F)C(=O)[C@]2(Cc2ccccn2)C1 10.1016/s0960-894x(02)00734-5
70682037 82656 20 None 43 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 495 5 0 8 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1 10.1016/j.bmcl.2013.07.044
CHEMBL2048820 82656 20 None 43 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 495 5 0 8 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1 10.1016/j.bmcl.2013.07.044
145948708 174275 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 886 20 7 10 5.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CNCCO3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL4299606 174275 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 886 20 7 10 5.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CNCCO3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
67410074 118514 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccc(C)n5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL3287216 118514 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccc(C)n5)ccc42)C3)nc1 10.1021/ml400473x
56926465 75815 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 4 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O 10.1021/jm2007062
CHEMBL1923613 75815 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 4 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O 10.1021/jm2007062
44434119 96681 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 400 10 3 10 -0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1nnn[nH]1 10.1016/j.bmcl.2007.07.099
CHEMBL237925 96681 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 400 10 3 10 -0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1nnn[nH]1 10.1016/j.bmcl.2007.07.099
70694648 82647 0 None - 1 Human 7.3 pKi = 7.3 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 462 7 0 7 3.6 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-c4nnc(C)o4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048811 82647 0 None - 1 Human 7.3 pKi = 7.3 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 462 7 0 7 3.6 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-c4nnc(C)o4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
155561671 182443 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 817 22 11 9 -0.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4581511 182443 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 817 22 11 9 -0.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
56926894 75839 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923638 75839 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
162672372 189865 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 656 14 3 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C=C/c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4794448 189865 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 656 14 3 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C=C/c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.9b02122
56925345 75844 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(F)ccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923643 75844 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(F)ccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
56926464 75814 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923612 75814 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)N(C)C1=O 10.1021/jm2007062
56942387 146440 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 579 13 4 7 4.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797857 146440 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 579 13 4 7 4.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL105462 215247 38 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm960054c
56926680 75825 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccccc2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923623 75825 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccccc2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
162649014 186720 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 702 14 4 7 6.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2c[nH]c3ccccc23)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4746362 186720 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 702 14 4 7 6.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2c[nH]c3ccccc23)cc1 10.1021/acs.jmedchem.9b02122
162666112 189093 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 638 13 3 8 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)c2ccc(C#N)nc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4784240 189093 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 638 13 3 8 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)c2ccc(C#N)nc2)cc1 10.1021/acs.jmedchem.9b02122
162676229 190083 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 715 15 3 10 3.9 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4797064 190083 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 715 15 3 10 3.9 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
58438475 99048 0 None 1548 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426677 99048 0 None 1548 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
58438475 99048 0 None 1548 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml400473x
CHEMBL2426677 99048 0 None 1548 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml400473x
56926461 75811 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923609 75811 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
118725956 123966 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 493 5 0 5 4.9 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)Cc4ccc(C5CC5)cn4)CC3)C2)ncn1 10.1021/ml500414n
CHEMBL3394195 123966 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 493 5 0 5 4.9 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)Cc4ccc(C5CC5)cn4)CC3)C2)ncn1 10.1021/ml500414n
155551597 180728 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 974 27 13 11 -1.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4541252 180728 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 974 27 13 11 -1.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
57394797 78060 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 461 5 0 7 4.7 Cc1nc2cnc(Oc3ccc(F)c4cccnc34)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957002 78060 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 461 5 0 7 4.7 Cc1nc2cnc(Oc3ccc(F)c4cccnc34)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
162649450 186833 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 725 14 3 10 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C2CCN(c3oc(C)nc3C#N)CC2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4747770 186833 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 725 14 3 10 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C2CCN(c3oc(C)nc3C#N)CC2)cc1 10.1021/acs.jmedchem.9b02122
58438464 9839 35 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
9060 9839 35 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
CHEMBL3287218 9839 35 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
DB14870 9839 35 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
58438464 9839 35 None 1 3 Human 8.2 pKi = 8.2 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
9060 9839 35 None 1 3 Human 8.2 pKi = 8.2 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
CHEMBL3287218 9839 35 None 1 3 Human 8.2 pKi = 8.2 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
DB14870 9839 35 None 1 3 Human 8.2 pKi = 8.2 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
67406334 118511 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 498 4 0 7 4.3 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN([C@@H]3CCc5cc(-c6ncccn6)ccc53)C4)nc2s1 10.1021/ml400473x
CHEMBL3287213 118511 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 498 4 0 7 4.3 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN([C@@H]3CCc5cc(-c6ncccn6)ccc53)C4)nc2s1 10.1021/ml400473x
57401798 78046 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 410 5 0 6 4.2 Cc1nc2ncc(Oc3ccc(F)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956989 78046 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 410 5 0 6 4.2 Cc1nc2ncc(Oc3ccc(F)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
58438475 99048 0 None 1548 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml500414n
CHEMBL2426677 99048 0 None 1548 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml500414n
11541319 75845 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 556 3 3 5 2.7 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2O1 10.1021/jm2007062
CHEMBL1923644 75845 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 556 3 3 5 2.7 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2O1 10.1021/jm2007062
162659375 188130 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 566 14 4 7 3.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNCC(=O)O)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4763077 188130 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 566 14 4 7 3.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNCC(=O)O)cc1 10.1021/acs.jmedchem.9b02122
127046807 146718 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799671 146718 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
127047654 146755 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799883 146755 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
121879 9015 24 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm960054c
5868 9015 24 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm960054c
CHEMBL308716 9015 24 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm960054c
162665952 189158 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 688 14 4 10 3.5 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4785149 189158 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 688 14 4 10 3.5 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
134139753 152814 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 5 3 5 2.5 CCCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3918783 152814 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 5 3 5 2.5 CCCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
162663868 188767 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 672 14 3 9 3.8 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4780408 188767 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 672 14 3 9 3.8 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
56926268 75792 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 542 4 3 5 2.5 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](Cc2ccccc2)C1=O 10.1021/jm2007062
CHEMBL1923510 75792 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 542 4 3 5 2.5 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](Cc2ccccc2)C1=O 10.1021/jm2007062
56926175 75788 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923504 75788 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
23635235 173280 0 None -239 5 Human 6.2 pKi = 6.2 Binding
Inhibition of ghrelin receptorInhibition of ghrelin receptor
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmc.2008.03.072
CHEMBL427860 173280 0 None -239 5 Human 6.2 pKi = 6.2 Binding
Inhibition of ghrelin receptorInhibition of ghrelin receptor
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmc.2008.03.072
70686292 82655 0 None - 1 Human 7.2 pKi = 7.2 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 461 5 0 8 3.0 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048819 82655 0 None - 1 Human 7.2 pKi = 7.2 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 461 5 0 8 3.0 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
90644554 118513 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ccncn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL3287215 118513 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ccncn5)ccc42)C3)nc1 10.1021/ml400473x
70682037 82656 20 None 43 2 Human 8.2 pKi = 8.2 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 495 5 0 8 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048820 82656 20 None 43 2 Human 8.2 pKi = 8.2 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 495 5 0 8 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1 10.1016/j.bmcl.2012.05.024
11664206 75828 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923626 75828 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
216208 16499 33 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1016/s0960-894x(02)00734-5
CHEMBL113313 16499 33 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1016/s0960-894x(02)00734-5
56926682 75827 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923625 75827 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
67408128 99055 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 5 0 6 3.4 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426684 99055 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 5 0 6 3.4 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
24180646 154961 0 None -1023 8 Human 6.1 pKi = 6.1 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1021/jm701137s
CHEMBL393576 154961 0 None -1023 8 Human 6.1 pKi = 6.1 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1021/jm701137s
57390496 75830 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
CHEMBL1923628 75830 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
CHEMBL501261 220914 23 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.8b01644
56926892 75837 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923636 75837 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
44434012 95849 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 479 13 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL236513 95849 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 479 13 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCc1ccccc1 10.1016/j.bmcl.2007.07.099
127046473 146558 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 661 17 6 8 4.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798645 146558 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 661 17 6 8 4.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
56942099 131972 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645256 131972 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
66601728 88616 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 514 5 2 4 4.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164499 88616 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 514 5 2 4 4.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
162657465 187820 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 652 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc[nH]2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4759418 187820 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 652 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc[nH]2)cc1 10.1021/acs.jmedchem.9b02122
56926891 75836 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 520 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923635 75836 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 520 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
44434015 95266 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 493 14 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL235011 95266 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 493 14 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCCc1ccccc1 10.1016/j.bmcl.2007.07.099
67407808 99058 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncc(C)cn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL2426687 99058 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncc(C)cn5)ccc42)C3)nc1 10.1021/ml400473x
56926173 75787 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923501 75787 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
3153998 74295 3 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 480 13 2 3 5.5 CCCC(C(=O)NC1CCCCC1)N(CCCN(CC)CC)C(=O)c1ccc(-c2ccccc2)[nH]1 10.1021/jm040103i
CHEMBL189561 74295 3 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 480 13 2 3 5.5 CCCC(C(=O)NC1CCCCC1)N(CCCN(CC)CC)C(=O)c1ccc(-c2ccccc2)[nH]1 10.1021/jm040103i
56926893 75838 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 10.1021/jm2007062
CHEMBL1923637 75838 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 10.1021/jm2007062
66788278 131970 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645254 131970 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
127045858 146640 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 618 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2=CCCCO2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799225 146640 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 618 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2=CCCCO2)cc1 10.1016/j.bmcl.2016.04.003
162677268 190352 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 663 14 3 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4800459 190352 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 663 14 3 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
58438487 99056 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 497 6 0 6 4.3 CCc1cnc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)Cc4ccc(OC)cn4)CC3)C2)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426685 99056 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 497 6 0 6 4.3 CCc1cnc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)Cc4ccc(OC)cn4)CC3)C2)nc1 10.1016/j.bmcl.2013.07.044
67407808 99058 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncc(C)cn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426687 99058 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncc(C)cn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
67407808 99058 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncc(C)cn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL2426687 99058 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncc(C)cn5)ccc42)C3)nc1 10.1021/ml400473x
67406727 123970 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 525 6 1 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
CHEMBL3394201 123970 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 525 6 1 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
162656896 187639 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 669 14 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2cccs2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4757313 187639 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 669 14 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2cccs2)cc1 10.1021/acs.jmedchem.9b02122
44579823 190860 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL482420 190860 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
44396320 73591 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 515 12 2 4 5.4 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccncc1 10.1021/jm040103i
CHEMBL186045 73591 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 515 12 2 4 5.4 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccncc1 10.1021/jm040103i
162674996 190168 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 522 12 3 6 4.2 CNCC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4798018 190168 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 522 12 3 6 4.2 CNCC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
44434111 153061 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1cc2ccccc2n1S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL392077 153061 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1cc2ccccc2n1S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
9745 9231 20 None - 0 Human 8.1 pIC50 = 8.1 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Drug Central 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 None
9804938 9231 20 None - 0 Human 8.1 pIC50 = 8.1 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Drug Central 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 None
CHEMBL278623 9231 20 None - 0 Human 8.1 pIC50 = 8.1 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Drug Central 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 None
DB13074 9231 20 None - 0 Human 8.1 pIC50 = 8.1 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Drug Central 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 None
9745 9231 20 None - 0 Human 7.8 pIC50 = 7.8 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Guide to Pharmacology 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 12240910
9804938 9231 20 None - 0 Human 7.8 pIC50 = 7.8 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Guide to Pharmacology 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 12240910
CHEMBL278623 9231 20 None - 0 Human 7.8 pIC50 = 7.8 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Guide to Pharmacology 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 12240910
DB13074 9231 20 None - 0 Human 7.8 pIC50 = 7.8 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Guide to Pharmacology 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 12240910
1102 8103 0 None - 1 Human 7.4 pKd = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12907757
1093 8575 0 None -12 2 Human 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
1093 8575 0 None -12 2 Human 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
4345065 8575 0 None -12 2 Human 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
4345065 8575 0 None -12 2 Human 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
1100 8389 45 None - 1 Human 7.9 pKd = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11061542
6918297 8389 45 None - 1 Human 7.9 pKd = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11061542
CHEMBL108335 8389 45 None - 1 Human 7.9 pKd = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11061542
1099 8568 0 None - 1 Human 9.0 pKd = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12907757
1099 8568 0 None - 1 Human 9.0 pKd = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
1092 9932 0 None - 1 Rat 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
134715446 9932 0 None - 1 Rat 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
2232 9932 0 None - 1 Rat 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
6918245 9932 0 None - 1 Rat 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
CHEMBL106593 9932 0 None - 1 Rat 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
58438464 9839 35 None -2 3 Mouse 8.1 pKi = 8.1 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
9060 9839 35 None -2 3 Mouse 8.1 pKi = 8.1 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
CHEMBL3287218 9839 35 None -2 3 Mouse 8.1 pKi = 8.1 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
DB14870 9839 35 None -2 3 Mouse 8.1 pKi = 8.1 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
58438464 9839 35 None -1 3 Rat 8.5 pKi = 8.5 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
9060 9839 35 None -1 3 Rat 8.5 pKi = 8.5 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
CHEMBL3287218 9839 35 None -1 3 Rat 8.5 pKi = 8.5 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
DB14870 9839 35 None -1 3 Rat 8.5 pKi = 8.5 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
58438464 9839 35 None 1 3 Human 8.9 pKi = 8.9 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cells.Measured <i>in vitro</i> in recombinant receptor over-expressing cells.
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
9060 9839 35 None 1 3 Human 8.9 pKi = 8.9 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cells.Measured <i>in vitro</i> in recombinant receptor over-expressing cells.
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
CHEMBL3287218 9839 35 None 1 3 Human 8.9 pKi = 8.9 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cells.Measured <i>in vitro</i> in recombinant receptor over-expressing cells.
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
DB14870 9839 35 None 1 3 Human 8.9 pKi = 8.9 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cells.Measured <i>in vitro</i> in recombinant receptor over-expressing cells.
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
12413 9844 0 None -3 2 Rat 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 4 1 8 4.3 CC1=CN2C=C(CC(=O)N3CCC4(CN(C4)[C@@H]5CCC6=CC(=CC=C56)C7=CC(C)=NC(O)=N7)CC3)N=C2S1 36631279
164946906 9844 0 None -3 2 Rat 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 4 1 8 4.3 CC1=CN2C=C(CC(=O)N3CCC4(CN(C4)[C@@H]5CCC6=CC(=CC=C56)C7=CC(C)=NC(O)=N7)CC3)N=C2S1 36631279
12413 9844 0 None 3 2 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 4 1 8 4.3 CC1=CN2C=C(CC(=O)N3CCC4(CN(C4)[C@@H]5CCC6=CC(=CC=C56)C7=CC(C)=NC(O)=N7)CC3)N=C2S1 36631279
164946906 9844 0 None 3 2 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 4 1 8 4.3 CC1=CN2C=C(CC(=O)N3CCC4(CN(C4)[C@@H]5CCC6=CC(=CC=C56)C7=CC(C)=NC(O)=N7)CC3)N=C2S1 36631279
23631116 10884 23 None - 1 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 5 0 5 4.8 Fc1ccc(cc1)Oc1ccc2c(c1)c(=O)n(c(n2)C)C[C@H]1CCCN(C1)C(C)C 17656463
3538 10884 23 None - 1 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 5 0 5 4.8 Fc1ccc(cc1)Oc1ccc2c(c1)c(=O)n(c(n2)C)C[C@H]1CCCN(C1)C(C)C 17656463
CHEMBL243001 10884 23 None - 1 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 5 0 5 4.8 Fc1ccc(cc1)Oc1ccc2c(c1)c(=O)n(c(n2)C)C[C@H]1CCCN(C1)C(C)C 17656463
1098 8173 0 None - 1 Rat 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11314756
1098 8173 0 None - 1 Rat 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14763915
1101 7444 0 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15339248
10740 8719 0 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 4 1 3 4.4 COc1ccc(c(c1Cl)Cl)[C@@H](NC(=O)N([C@@H]1CCN(CC1(C)C)C)C)C 25327342
146170991 8719 0 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 4 1 3 4.4 COc1ccc(c(c1Cl)Cl)[C@@H](NC(=O)N([C@@H]1CCN(CC1(C)C)C)C)C 25327342
1092 9932 0 None - 1 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
134715446 9932 0 None - 1 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
2232 9932 0 None - 1 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
6918245 9932 0 None - 1 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
CHEMBL106593 9932 0 None - 1 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
178024 8752 33 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10427162
5867 8752 33 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10427162
CHEMBL13817 8752 33 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10427162
1099 8568 0 None - 1 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11314756
1093 8575 0 None 12 2 Rat 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
4345065 8575 0 None 12 2 Rat 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793