Ligand source activities (1 row/activity)





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 183275 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 183275 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 162277 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 162277 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 177083 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 177083 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 94063 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 94063 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 176649 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 176649 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 177083 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 177083 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 94063 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 94063 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 183298 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 183298 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 176649 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 176649 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 154416 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 154416 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 176826 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 176826 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 190504 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 190504 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 95449 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 95449 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 158851 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 158851 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 158865 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 158865 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 176826 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 176826 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 177232 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 177232 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 176998 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 176998 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 177232 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 177232 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 183406 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 183406 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 176223 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 176223 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 176998 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 176998 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 10229 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 10229 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 10229 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 10229 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 97120 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 97120 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 177531 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 177531 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 183467 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 183467 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 88579 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 88579 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 177531 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 177531 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 109230 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 109230 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 193187 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 193187 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 1940 30 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 1940 30 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 1940 30 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 176898 4 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 176898 4 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 176910 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 176910 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 95768 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 95768 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 190844 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 190844 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 88537 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 88537 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 1940 30 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 1940 30 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 1940 30 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 97352 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 97352 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 155063 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 155063 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 94550 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 94550 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 176898 4 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 176898 4 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 176910 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 176910 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 166323 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 166323 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 177417 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 177417 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 63134 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 63134 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 63311 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 63311 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 63311 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 63311 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 63311 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 63311 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 122303 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 122303 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 122303 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 122303 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 155016 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 155016 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 94000 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 94000 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 176716 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 176716 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 177417 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 177417 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 97537 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 97537 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 182987 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 182987 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 88539 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 88539 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 88584 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 88584 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 155022 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 155022 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 176716 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 176716 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 160013 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 160013 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 94817 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 94817 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 10218 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 10218 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 78750 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 78750 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 10218 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 10218 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 154539 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 154539 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 88463 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 88463 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 158913 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 158913 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 131266 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 131266 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 160554 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 160554 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 94578 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 94578 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 62762 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 62762 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 177515 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 177515 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 93545 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 93545 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 104081 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 104081 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 138745 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 138745 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 176807 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 176807 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 177515 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 177515 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 97579 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 97579 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 156758 1 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 156758 1 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 156758 1 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 156758 1 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 88517 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 88517 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 154793 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 154793 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 104081 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 104081 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 138745 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 138745 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 139237 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 139237 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 177632 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 177632 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 176807 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 176807 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 63126 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 63126 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 178523 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 178523 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 9635 27 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 9635 27 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 96027 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 96027 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 9635 27 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 9635 27 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 177481 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 177481 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 10227 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 10227 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 182435 3 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 182435 3 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 177339 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 177339 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 177481 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 177481 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 177629 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 177629 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 177632 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 177632 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 68671 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 68671 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 68677 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 68677 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 68694 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 68694 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 68695 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 68695 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 68702 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 68702 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 68711 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 68711 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 68722 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 68722 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 68726 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 68726 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 71258 13 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 71258 13 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 71258 13 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 141841 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 141841 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 142294 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 142294 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 142605 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 142605 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 142921 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 142921 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 142973 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 142973 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 143162 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 143162 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 143606 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 143606 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 143836 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 143836 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 144034 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 144034 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 144330 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 144330 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 144399 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 144399 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 144754 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 144754 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 144793 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 144793 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 144853 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 144853 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 145041 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 145041 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 145227 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 145227 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 145404 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 145404 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 145658 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 145658 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 145840 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 145840 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 145914 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 145914 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 146021 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 146021 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 146585 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 146585 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 147219 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 147219 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 147222 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 147222 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 147482 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 147482 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 147822 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 147822 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 147942 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 147942 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 148254 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 148254 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 148558 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 148558 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 148957 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 148957 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 150482 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 150482 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 150560 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 150560 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 151871 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 151871 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 152188 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 152188 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 189665 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 189665 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 89310 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 89310 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 88447 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 88447 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 88462 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 88462 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 88491 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 88491 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 88512 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 88512 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 161265 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 161265 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 177339 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 177339 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 177629 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 177629 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 10212 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 10212 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 10212 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 10212 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 94523 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 94523 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 155023 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 155023 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 27125 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 27125 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 97889 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 97889 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 162143 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 162143 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 189245 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 189245 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 88534 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 88534 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 88543 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 88543 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 94494 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 94494 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 95871 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 95871 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 1940 30 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 1940 30 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 1940 30 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 1940 30 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 1940 30 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 1940 30 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 1940 30 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 1940 30 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 1940 30 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 162143 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 162143 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 95357 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 95357 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 212344 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 212344 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 63494 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 63494 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 212344 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 179963 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 179963 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 212344 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 212344 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 1940 30 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 1940 30 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 1940 30 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 176724 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 176724 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 63973 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 63973 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 64285 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 64285 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 64285 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 64285 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 16197 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 16197 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 211583 15 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 211583 15 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 161751 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 161751 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 203590 0 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 203590 0 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 176724 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 176724 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 176915 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 176915 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 88490 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 88490 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 88493 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 88493 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 88536 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 88536 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 88541 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 88541 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 88587 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 88587 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 190700 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 190700 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 96486 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 96486 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 203590 0 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 203590 0 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 91118 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 91118 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 94551 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 94551 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 94524 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 94524 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 206726 34 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 94436 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 94436 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 95899 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 95899 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 23889 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 23889 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 27280 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 27280 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 112488 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 112488 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 23889 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 23889 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 176480 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 176480 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 153433 7 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 153433 7 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 153433 7 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 153433 7 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 153433 7 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 153433 7 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 153433 7 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 153433 7 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 10227 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 10227 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 100755 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 100755 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 176480 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 176480 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 176761 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 176761 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 177007 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 177007 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 95810 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 95810 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 97138 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 97138 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 183377 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 183377 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 88508 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 88508 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 88516 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 88516 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 88552 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 88552 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 88592 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 88592 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 186186 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 186186 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 93585 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 93585 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 161525 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 161525 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 162226 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 162226 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 89477 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 89477 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 5264 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 5264 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 10209 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 10209 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 10226 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 10226 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 100619 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 100619 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 100619 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 139250 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 139250 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 176760 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 176760 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 177056 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 177056 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 94937 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 94937 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 183464 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 183464 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 206726 34 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 88452 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 88452 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 88467 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 88467 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 88468 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 88468 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 88486 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 88486 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 88499 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 88499 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 88542 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 88542 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 88555 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 88555 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 88589 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 88589 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 88591 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 88591 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 147587 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 147587 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 177056 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 177056 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 166764 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 166764 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 176760 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 176760 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 162392 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 162392 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 168816 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 168816 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 96235 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 96235 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 97365 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 97365 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 158788 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 158788 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 68713 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 68713 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 68715 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 68715 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 68718 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 68718 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 68720 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 68720 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 68721 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 68721 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 141936 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 141936 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 142704 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 142704 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 143859 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 143859 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 144128 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 144128 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 144438 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 144438 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 144927 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 144927 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 146196 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 146196 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 147921 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 147921 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 148248 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 148248 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 148502 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 148502 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 150480 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 150480 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 150810 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 150810 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 151016 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 151016 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 151547 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 151547 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 151583 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 151583 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 151838 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 151838 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 152293 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 152293 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 152785 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 152785 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 153117 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 153117 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 178804 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 178804 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 212451 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 212451 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 212451 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 212451 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 210019 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 210022 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 88473 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 88473 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 88475 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 88475 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 88484 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 88484 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 88485 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 88485 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 88506 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 88506 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 88523 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 88523 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 88527 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 88527 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 88545 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 88545 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 88574 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 88574 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 190748 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 190748 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 177514 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 177514 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 145503 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 145503 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 95891 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 95891 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 177514 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 177514 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 88084 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 88084 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 210022 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 95327 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 95327 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 136684 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 136684 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 68711 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 68711 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 207623 13 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 207623 13 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 63983 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 63983 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 88985 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 88985 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 146325 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 146325 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 166707 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 166707 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 207618 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 89600 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 89600 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 91121 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 91121 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 141079 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 141079 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 94239 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 94239 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 63987 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 63987 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 207623 13 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 207623 13 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 177235 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 177235 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 162384 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 162384 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 176666 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 176666 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 177235 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 177235 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 88445 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 88445 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 88496 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 88496 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 88528 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 88528 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 88544 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 88544 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 88562 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 88562 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 88569 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 88569 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 88595 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 88595 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 88598 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 88598 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 207621 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 183528 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 183528 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 186255 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 186255 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 192918 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 192918 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 192019 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 192019 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 166197 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 166197 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 177192 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 177192 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 207619 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 187784 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 187784 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 154148 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 154148 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 161500 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 161500 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 161974 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 161974 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 162179 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 162179 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 176658 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 176658 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 95881 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 95881 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 88458 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 88458 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 88466 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 88466 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 177192 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 177192 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 184168 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 184168 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 166660 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 166660 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 162179 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 162179 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 112344 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 112344 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 64254 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 64254 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 207625 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 207621 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 176666 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 176666 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 176658 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 176658 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 68670 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 68670 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 147498 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 147498 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 170469 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 170469 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 161500 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 161500 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 161974 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 161974 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 154793 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 154793 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 68702 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 68702 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 162384 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 162384 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 145748 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 145748 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 97818 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 97818 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 97818 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 146486 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 146486 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 97818 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 97818 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 97818 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 97818 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 97818 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 97818 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 168816 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 168816 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 182440 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 182440 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 64019 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 64019 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 147341 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 147341 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 159846 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 159846 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 183646 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 183646 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 186412 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 186412 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 96137 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 96137 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 136699 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 136699 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 186377 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 186377 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 90528 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 90528 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 89347 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 89347 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 161951 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 161951 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 78753 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 78753 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 84512 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 84512 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 180459 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 180459 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 93586 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 93586 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 161951 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 161951 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 96472 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 96472 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 154686 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 154686 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 183299 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 183299 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 183373 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 183373 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 88446 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 88446 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 88455 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 88455 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 88457 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 88457 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 88469 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 88469 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 88477 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 88477 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 88489 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 88489 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 88497 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 88497 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 88501 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 88501 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 88558 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 88558 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 88588 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 88588 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 88600 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 88600 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 186401 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 186401 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 154719 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 154719 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 168294 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 168294 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 186291 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 186291 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 161936 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 161936 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 88230 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 88230 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 180809 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 180809 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 93966 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 93966 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 162256 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 162256 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 162453 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 162453 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 176781 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 176781 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 159031 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 159031 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 5636 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 5636 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 88480 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 88480 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 88601 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 88601 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 154852 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 154852 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 161936 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 161936 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 5635 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 5635 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 154140 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 154140 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 98007 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 98007 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 96096 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 96096 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 162219 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 162219 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 162219 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 68697 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 68697 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 172388 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 172388 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 10228 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 10228 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 162453 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 162453 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 207626 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 147150 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 147150 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 176781 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 176781 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 207612 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 89481 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 89481 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 89481 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 89481 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 10228 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 10228 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 162219 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 162219 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 162219 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 167821 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 167821 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 122805 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 122805 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 207622 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 162256 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 162256 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 139101 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 139101 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 139590 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 139590 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 200833 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 200833 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 137489 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 137489 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 68706 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 68706 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 174015 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 174015 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 98792 12 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 98792 12 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 139590 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 139590 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 200833 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 200833 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 186320 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 186320 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 145483 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 145483 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 207613 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 89081 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 89081 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 166218 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 166218 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 210013 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 162037 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 162037 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 97154 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 97154 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 97200 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 97200 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 97386 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 97386 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 29827 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 29827 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 179949 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 179949 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 161406 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 161406 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 11927 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 11927 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 11927 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 64536 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 64536 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 167750 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 167750 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 94036 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 94036 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 161614 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 161614 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 162037 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 162037 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 162174 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 162174 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 162474 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 162474 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 97094 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 97094 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 5767 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 5767 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 183376 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 183376 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 88449 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 88449 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 88482 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 88482 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 88502 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 88502 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 88513 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 88513 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 88532 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 88532 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 88546 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 88546 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 88551 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 88551 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 88554 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 88554 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 88559 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 88559 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 88576 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 88576 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 88582 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 88582 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 88583 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 88583 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 64535 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 64535 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 166791 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 166791 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 177072 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 177072 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 210013 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 190862 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 190862 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 161751 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 161751 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 10211 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 10211 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 100755 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 100755 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 176915 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 176915 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 63606 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 63606 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 63606 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 63606 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 16925 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 16925 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 177007 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 177007 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 176761 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 176761 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 10208 0 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 10208 0 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 10208 0 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 10208 0 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 64338 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 64338 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 207610 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 176734 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 176734 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 112895 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 112895 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 112895 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 112895 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 78752 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 78752 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 64305 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 64305 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 64543 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 64543 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 91582 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 91582 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 174015 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 174015 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 94064 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 94064 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 161729 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 161729 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 10211 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 10211 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 176691 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 176691 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 176734 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 176734 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 97479 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 97479 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 183254 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 183254 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 88488 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 88488 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 88511 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 88511 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 88524 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 88524 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 88538 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 88538 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 88593 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 88593 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 10213 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 10213 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 10213 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 10213 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 167504 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 167504 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 207623 13 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 207623 13 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 176691 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 176691 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 167504 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 167504 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 177368 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 177368 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 95774 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 95774 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 97774 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 97774 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 184166 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 184166 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 186465 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 186465 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 186483 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 186483 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 88221 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 88221 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 139331 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 139331 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 68702 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 68702 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 23858 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 23858 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 113295 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 113295 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 123392 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 123392 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 186341 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 186341 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 88064 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 88064 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 186314 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 186314 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 186553 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 186553 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 190755 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 190755 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 97200 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 97200 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 158105 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 158105 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 177072 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 177072 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 161614 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 161614 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 162174 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 162174 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 162474 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 162474 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 64126 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 64126 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 64130 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 64130 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 113744 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 113744 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 179146 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 179146 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 187603 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 187603 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 137610 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 137610 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 166156 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 166156 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 62619 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 62619 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 154600 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 154600 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 187603 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 187603 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 172388 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 172388 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 186578 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 186578 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 189827 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 189827 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 161716 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 161716 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 162445 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 162445 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 158157 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 158157 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 158833 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 158833 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 96503 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 96503 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 68695 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 68695 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 180637 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 180637 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 161608 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 161608 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 207623 13 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 207623 13 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 94120 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 94120 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 154835 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 154835 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 16028 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 16028 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 207614 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 154719 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 154719 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 154984 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 154984 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 162165 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 162165 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 30270 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 30270 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 179900 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 179900 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 176697 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 176697 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 161763 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 161763 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 162165 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 162165 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 162445 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 162445 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 176697 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 176697 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 177460 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 177460 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 88453 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 88453 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 88478 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 88478 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 88492 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 88492 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 88505 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 88505 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 88509 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 88509 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 88519 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 88519 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 88521 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 88521 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 88531 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 88531 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 88556 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 88556 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 88563 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 88563 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 177460 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 177460 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 188314 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 188314 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 161514 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 161514 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 161514 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 161514 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 161608 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 161608 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 161716 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 161716 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 161985 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 161985 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 162186 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 162186 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 210018 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 91373 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 91373 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 63967 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 63967 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 131581 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 131581 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 88986 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 88986 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 159203 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 159203 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 68722 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 68722 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 128281 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 128281 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 186187 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 186187 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 162186 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 162186 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 210018 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 71258 13 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 71258 13 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 71258 13 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 158690 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 158690 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 88645 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 88645 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 97149 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 97149 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 68726 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 68726 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 63533 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 63533 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 181198 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 181198 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 172388 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 172388 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 161985 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 161985 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 78742 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 78742 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 161763 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 161763 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 179361 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 179361 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 145017 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 145017 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 71258 13 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 71258 13 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 71258 13 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 120750 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 120750 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 166090 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 166090 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 207623 13 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 207623 13 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 148073 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 148073 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 166028 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 166028 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 183499 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 183499 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 161729 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 161729 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 162226 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 162226 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 158284 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 158284 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 10225 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 10225 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 77391 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 77391 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 98792 12 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 98792 12 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 140679 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 140679 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 206945 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 96486 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 96486 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 96486 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 96486 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 153642 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 153642 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 15402 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 15402 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 10225 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 10225 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 77391 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 77391 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 98792 12 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 98792 12 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 140679 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 140679 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 206945 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 176804 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 176804 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 96167 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 96167 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 94458 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 94458 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 154229 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 154229 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 176804 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 176804 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 177368 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 177368 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 191962 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 191962 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 88535 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 88535 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 88571 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 88571 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 88597 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 88597 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 88603 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 88603 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 95412 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 95412 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 89312 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 89312 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 207623 13 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 207623 13 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 63307 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 63307 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 122482 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 122482 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 207623 13 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 207623 13 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 182249 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 182249 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 89162 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 89162 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 207623 13 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 207623 13 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 93544 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 93544 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 76908 0 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 76908 0 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 176849 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 176849 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 94823 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 94823 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 154489 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 154489 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 5765 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 5765 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 5766 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 5766 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 190711 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 190711 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 88483 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 88483 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 88522 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 88522 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 88533 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 88533 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 88570 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 88570 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 88585 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 88585 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 88594 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 88594 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 88278 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 88278 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 186253 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 186253 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 191955 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 191955 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 88345 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 88345 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 88278 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 88278 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 88278 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 88278 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 88345 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 88345 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 200408 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 200408 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 200832 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 200832 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 200408 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 200408 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 200832 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 200832 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 94818 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 94818 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 166724 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 166724 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 154415 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 154415 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 161965 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 161965 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 183374 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 183374 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 189379 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 189379 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 120750 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 120750 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 88448 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 88448 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 88454 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 88454 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 88456 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 88456 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 88487 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 88487 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 88495 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 88495 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 88503 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 88503 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 88514 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 88514 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 88525 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 88525 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 88526 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 88526 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 88547 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 88547 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 88550 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 88550 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 88557 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 88557 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 88564 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 88564 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 88578 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 88578 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 88602 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 88602 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 68716 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 68716 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 177550 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 177550 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 177076 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 177076 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 177550 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 177550 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 94650 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 94650 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 154554 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 154554 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 182846 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 182846 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 210017 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 177076 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 177076 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 88988 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 88988 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 161343 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 161343 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 94210 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 94210 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 212344 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 95358 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 95358 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 94459 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 94459 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 192468 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 192468 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 210017 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 94437 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 94437 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 89476 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 89476 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 161965 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 161965 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 89478 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 89478 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 179156 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 179156 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 15378 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 15378 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 161735 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 161735 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 98212 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 98212 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 68720 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 68720 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 165838 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 165838 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 173377 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 173377 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 96730 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 96730 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 96770 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 96770 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 11159 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 11159 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 11159 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 68677 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 68677 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 63997 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 63997 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 167214 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 167214 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 161707 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 161707 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 161735 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 161735 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 177553 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 177553 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 94938 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 94938 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 95773 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 95773 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 96092 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 96092 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 96266 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 96266 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 154711 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 154711 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 210021 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 88479 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 88479 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 88494 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 88494 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 88498 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 88498 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 88510 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 88510 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 88568 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 88568 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 88572 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 88572 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 88875 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 88875 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 152523 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 152523 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 191964 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 191964 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 88459 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 88459 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 186319 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 186319 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 137353 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 137353 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 145750 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 145750 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 76908 0 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 76908 0 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 139036 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 139036 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 137353 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 137353 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 95328 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 95328 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 64514 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 64514 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 176849 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 176849 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 95566 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 95566 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 166936 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 166936 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 99184 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 99184 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 99184 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 99184 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 10206 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 10206 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 176994 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 176994 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 10206 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 10206 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 64282 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 64282 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 186597 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 186597 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 188515 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 188515 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 192464 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 192464 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 160555 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 160555 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 68696 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 68696 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 166024 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 166024 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 186313 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 186313 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 186408 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 186408 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 136585 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 136585 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 122485 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 122485 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 210021 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 168478 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 168478 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 154135 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 154135 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 166893 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 166893 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 23666 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 23666 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 181797 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 181797 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 144462 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 144462 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 88147 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 88147 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 177553 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 177553 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 122093 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 122093 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 11917 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 11917 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 11917 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 166111 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 166111 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 161707 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 161707 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 186387 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 186387 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 114880 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 114880 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 11157 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 11157 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 11157 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 137287 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 137287 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 123038 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 123038 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 182991 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 182991 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 16290 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 16290 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 146039 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 146039 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 212451 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 212451 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 191061 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 191061 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 170874 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 170874 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 161506 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 161506 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 171750 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 171750 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 165983 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 165983 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 165920 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 165920 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 89762 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 89762 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 136712 0 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 136712 0 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 68714 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 68714 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 207620 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 162112 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 162112 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 10217 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 10217 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 137661 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 137661 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 139006 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 139006 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 168718 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 168718 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 71258 13 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 71258 13 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 71258 13 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 15355 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 15355 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 16672 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 16672 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 176549 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 176549 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 94035 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 94035 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 162112 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 162112 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 10217 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 10217 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 137661 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 137661 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 139006 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 139006 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 168718 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 168718 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 176549 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 176549 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 176994 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 176994 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 189576 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 189576 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 88451 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 88451 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 88474 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 88474 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 88476 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 88476 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 88515 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 88515 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 88530 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 88530 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 88567 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 88567 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 88599 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 88599 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 78747 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 78747 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 78751 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 78751 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 147339 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 147339 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 207623 13 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 207623 13 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 10207 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 10207 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 62195 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 62195 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 10207 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 10207 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 207624 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 186342 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 186342 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 186436 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 186436 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 180535 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 180535 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 161506 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 161506 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 162290 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 162290 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 88470 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 88470 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 88471 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 88471 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 88472 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 88472 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 88520 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 88520 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 88573 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 88573 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 88586 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 88586 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 88596 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 88596 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 192647 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 192647 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 147331 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 147331 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 68713 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 68713 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 166591 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 166591 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 148323 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 148323 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 162290 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 162290 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 159398 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 159398 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 68718 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 68718 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 89480 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 89480 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 146001 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 146001 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 10216 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 10216 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 30233 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 30233 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 10216 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 10216 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 88063 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 88063 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 10215 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 10215 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 100771 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 100771 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 78743 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 78743 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 182722 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 182722 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 210012 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 112590 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 112590 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 10215 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 10215 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 10226 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 10226 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 100771 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 100771 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 145123 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 145123 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 177569 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 177569 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 116512 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 116512 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 116512 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 116512 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 177569 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 177569 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 160761 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 160761 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 191989 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 191989 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 210012 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 88461 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 88461 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 88500 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 88500 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 88504 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 88504 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 88560 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 88560 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 88577 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 88577 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 88580 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 88580 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 88604 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 88604 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 121632 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 121632 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 166896 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 166896 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 207621 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 94577 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 94577 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 186482 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 186482 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 166935 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 166935 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 2204 19 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 2204 19 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 2204 19 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 165910 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 165910 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 120751 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 120751 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 183690 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 183690 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 155016 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 155016 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 182927 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 182927 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 207615 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 154230 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 154230 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 177334 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 177334 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 97364 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 97364 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 120751 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 120751 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 210014 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 88450 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 88450 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 88460 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 88460 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 88561 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 88561 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 88575 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 88575 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 162241 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 162241 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 136700 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 136700 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 96899 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 96899 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 162241 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 162241 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 177003 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 177003 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 94982 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 94982 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 5678 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 5678 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 166519 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 166519 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 94817 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 94817 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 136196 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 136196 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 136196 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 136196 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 29207 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 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 29207 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 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 3638 31 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 3638 31 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 3638 31 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 3638 31 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 3638 31 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 175091 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 175091 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 89170 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 89170 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 166143 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 166143 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 68670 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 68670 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 11170 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 11170 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 11170 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 177003 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 177003 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 177334 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 177334 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 11929 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 11929 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 11929 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 186241 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 186241 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 161635 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 161635 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 177057 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 177057 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 207621 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 207623 13 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 207623 13 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 63169 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 63169 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 63990 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 63990 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 140805 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 140805 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 140805 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 140805 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 96094 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 96094 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 63311 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 63311 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 63574 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 63574 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 177649 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 177649 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 78754 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 78754 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 89472 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 89472 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 161635 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 161635 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 176506 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 176506 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 176928 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 176928 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 177057 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 177057 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 177649 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 177649 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 183351 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 183351 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 183465 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 183465 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 88465 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 88465 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 88481 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 88481 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 88507 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 88507 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 88548 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 88548 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 88553 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 88553 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 88565 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 88565 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 88590 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 88590 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 11946 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 11946 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 11946 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 95854 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 95854 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 139164 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 139164 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 139164 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 139164 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 166653 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 166653 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 210014 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 214062 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 96565 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 96565 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 181406 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 181406 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 165899 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 165899 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 189985 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 189985 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 139533 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 139533 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 147646 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 147646 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 94184 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 94184 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 161735 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 161735 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 174015 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 174015 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 68721 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 68721 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 200407 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 200407 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 200407 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 200407 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 186254 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 186254 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 147650 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 147650 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 147650 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 147650 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 161735 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 161735 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 5779 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 5779 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 5901 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 5901 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 210020 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 88464 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 88464 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 88518 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 88518 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 88549 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 88549 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 88566 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 88566 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 159231 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 159231 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 112383 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 112383 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 68712 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 68712 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 179474 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 179474 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 176928 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 176928 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 160108 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 160108 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 10210 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 10210 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 10214 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 10214 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 10210 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 10210 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 10214 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 10214 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 180278 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 180278 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 145620 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 145620 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 176506 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 176506 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 167391 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 167391 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 192648 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 192648 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 139206 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 139206 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 89311 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 89311 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 68671 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 68671 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 166281 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 166281 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 68724 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 68724 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 166587 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 166587 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 88874 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 88874 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 154584 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 154584 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 210020 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 179258 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 179258 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 63954 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 63954 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 167391 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 167391 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 19253 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 19253 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 207611 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 89473 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 89473 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 63585 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 63585 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 78748 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 78748 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 184170 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 184170 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 186189 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 186189 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 191926 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 191926 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 186360 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 186360 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 186252 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 186252 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 166262 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 166262 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 166375 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 166375 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 207617 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 166339 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 166339 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 84422 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 84422 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 212364 19 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 144919 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 144919 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 144917 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 144917 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 210019 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 210416 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 97775 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 97775 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 72853 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 72853 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 96486 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 96486 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 213804 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 112981 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 112981 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 81438 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 81438 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 72854 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 72854 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 112942 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 112942 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 76991 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 76991 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 64900 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 64900 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 77297 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 77297 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 75640 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 75640 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 122721 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 122721 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 140793 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 140793 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 139410 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 139410 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 5459 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 5459 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 121488 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 121488 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 120825 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 120825 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 66337 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 66337 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 123514 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 123514 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 121518 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 121518 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 166837 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 166837 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 79806 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 79806 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 120834 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 120834 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 77563 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 77563 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 138712 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 138712 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 76371 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 76371 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 72845 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 72845 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 76380 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 76380 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 75204 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 75204 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 75216 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 75216 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 81435 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 81435 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 81489 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 81489 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 81496 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 81496 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 120835 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 120835 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 212662 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 139132 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 139132 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 166406 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 166406 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 65831 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 65831 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 139442 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 139442 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 81425 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 81425 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 166218 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 166218 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 81427 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 81427 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 74651 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 74651 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 6190 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 6190 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 72856 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 72856 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 76414 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 76414 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 7516 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 7516 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 5834 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 5834 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 74664 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 74664 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 166587 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 166587 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 139403 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 139403 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 120836 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 120836 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 165983 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 165983 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 6300 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 6300 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 120838 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 120838 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 166660 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 166660 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 81439 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 81439 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 6068 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 6068 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 121495 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 121495 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 75989 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 75989 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 139189 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 139189 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 166193 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 166193 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 139442 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 139442 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 6028 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 6028 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 160767 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 160767 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 74338 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 74338 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 140315 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 140315 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 75905 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 75905 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 81493 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 81493 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 213804 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 62663 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 62663 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 75621 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 75621 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 75643 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 75643 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 6181 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 6181 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 81492 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 81492 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 140315 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 140315 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 75828 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 75828 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 5921 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 5921 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 72851 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 72851 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 66677 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 66677 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 210054 4 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 6310 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 6310 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 81424 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 81424 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 166313 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 166313 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 126304 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 126304 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 213804 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 213804 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 213804 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 139447 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 139447 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 166762 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 166762 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 166764 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 166764 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 212181 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 75635 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 75635 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 64129 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 64129 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 72860 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 72860 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 213804 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 120834 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 120834 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 6066 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 6066 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 140478 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 140478 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 62247 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 62247 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 72848 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 72848 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 166143 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 166143 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 66008 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 66008 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 212364 19 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 62669 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 62669 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 165373 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 165373 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 165373 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 165373 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 62669 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 62669 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 75346 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 75346 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 166111 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 166111 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 140686 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 140686 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 78363 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 78363 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 62663 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 62663 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 124538 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 124538 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 74651 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 74651 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 75676 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 75676 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 124677 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 124677 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 75829 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 75829 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 212451 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 212451 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 65855 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 65855 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 75581 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 75581 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 139410 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 139410 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 136503 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 136503 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 166724 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 166724 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 120824 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 120824 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 72857 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 72857 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 124673 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 124673 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 124675 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 124675 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 139427 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 139427 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 124672 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 124672 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 139427 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 139427 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 72879 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 72879 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 5955 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 5955 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 120828 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 120828 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 5981 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 5981 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 120828 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 120828 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 72859 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 72859 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 72861 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 72861 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 212451 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 212451 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 120830 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 120830 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 6058 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 6058 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 6067 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 6067 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 72878 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 72878 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 166738 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 166738 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 120833 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 120833 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 75534 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 75534 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 212451 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 212451 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 212349 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 76391 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 76391 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 120836 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 120836 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 81426 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 81426 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 124677 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 124677 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 75176 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 75176 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 81428 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 81428 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 120823 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 120823 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 76287 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 76287 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 120837 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 120837 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 64542 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 64542 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 166451 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 166451 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 166402 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 166402 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 137871 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 137871 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 81433 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 81433 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 81498 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 81498 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 166653 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 166653 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 6299 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 6299 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 75513 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 75513 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 77531 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 77531 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 120833 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 120833 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 6158 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 6158 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 81434 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 81434 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 121520 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 121520 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 62176 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 62176 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 81500 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 81500 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 81490 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 81490 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 75046 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 75046 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 6112 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 6112 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 72850 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 72850 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 212212 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 212451 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 212451 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 166842 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 166842 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 81494 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 81494 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 137151 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 137151 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 81437 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 81437 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 213804 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 72849 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 72849 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 6292 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 6292 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 62270 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 62270 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 166707 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 166707 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 140722 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 140722 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 166028 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 166028 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 64129 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 64129 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 212451 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 212451 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 168987 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 168987 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 166262 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 166262 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 65807 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 65807 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 124672 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 124672 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 124674 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 124674 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 124676 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 124676 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 139332 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 139332 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 72847 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 72847 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 72881 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 72881 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 138006 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 138006 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 75654 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 75654 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 166375 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 166375 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 64873 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 64873 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 75533 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 75533 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 121073 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 121073 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 7531 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 7531 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 121654 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 121654 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 72863 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 72863 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 120837 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 120837 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 72855 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 72855 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 166024 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 166024 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 76182 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 76182 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 75906 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 75906 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 123862 1 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 123862 1 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 76319 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 76319 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 75672 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 75672 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 212451 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 212451 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 74072 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 74072 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 139447 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 139447 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 168148 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 168148 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 165899 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 165899 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 124678 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 124678 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 5833 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 5833 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 75848 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 75848 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 120822 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 120822 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 7515 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 7515 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 138725 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 138725 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 121494 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 121494 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 140187 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 140187 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 140974 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 140974 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 75157 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 75157 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 76389 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 76389 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 75616 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 75616 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 212451 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 212451 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 139413 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 139413 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 75199 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 75199 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 166791 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 166791 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 74651 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 74651 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 5832 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 5832 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 81431 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 81431 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 140833 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 140833 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 165273 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 165273 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 140720 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 140720 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 79491 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 79491 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 167775 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 167775 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 139084 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 139084 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 139177 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 139177 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 139332 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 139332 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 124673 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 124673 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 139177 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 139177 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 6021 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 6021 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 72862 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 72862 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 120820 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 120820 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 120830 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 120830 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 138768 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 138768 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 5552 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 5552 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 76790 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 76790 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 166363 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 166363 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 120838 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 120838 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 79807 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 79807 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 213804 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 64283 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 64283 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 139285 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 139285 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 139403 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 139403 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 120822 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 120822 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 76372 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 76372 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 7530 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 7530 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 6130 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 6130 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 120826 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 120826 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 139132 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 139132 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 212451 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 212451 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 76353 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 76353 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 123336 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 123336 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 165920 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 165920 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 5918 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 5918 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 81436 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 81436 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 81491 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 81491 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 62616 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 62616 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 77000 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 77000 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 76796 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 76796 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 64245 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 64245 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 66742 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 66742 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 210054 4 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 120831 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 120831 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 75684 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 75684 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 140804 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 140804 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 72876 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 72876 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 83116 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 83116 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 120824 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 120824 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 62584 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 62584 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 168081 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 168081 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 81501 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 81501 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 138007 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 138007 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 165838 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 165838 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 126246 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 126246 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 74499 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 74499 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 166339 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 166339 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 123869 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 123869 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 79478 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 79478 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 66000 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 66000 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 65871 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 65871 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 166385 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 166385 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 75450 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 75450 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 76164 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 76164 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 166197 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 166197 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 6311 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 6311 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 72877 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 72877 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 120820 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 120820 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 213804 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 112950 13 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 112950 13 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 75632 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 75632 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 124678 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 124678 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 212451 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 212451 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 136512 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 136512 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 62749 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 62749 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 212451 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 212451 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 74715 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 74715 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 141268 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 141268 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 62175 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 62175 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 123340 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 123340 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 6065 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 6065 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 81432 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 81432 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 6191 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 6191 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 5944 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 5944 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 6294 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 6294 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 140836 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 140836 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 120826 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 120826 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 6293 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 6293 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 212379 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 166090 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 166090 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 64284 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 64284 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 75148 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 75148 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 75438 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 75438 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 75615 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 75615 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 218 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 218 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 218 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 79192 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 79192 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 120827 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 120827 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 139084 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 139084 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 6119 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 6119 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 81429 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 81429 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 72846 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 72846 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 72880 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 72880 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 72844 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 72844 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 165484 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 165484 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 165484 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 165484 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 120831 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 120831 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 120832 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 120832 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 139413 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 139413 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 139231 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 139231 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 76981 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 76981 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 81499 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 81499 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 126652 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 126652 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 76057 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 76057 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 81497 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 81497 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 120790 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 120790 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 76700 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 76700 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 64252 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 64252 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 122723 33 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 122723 33 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 6309 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 6309 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 120825 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 120825 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 140029 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 140029 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 75029 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 75029 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 169466 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 169466 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 72852 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 72852 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 120835 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 120835 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 75644 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 75644 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 166519 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 166519 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 123948 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 123948 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 124674 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 124674 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 124675 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 124675 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 123948 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 123948 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 72844 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 72844 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 72858 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 72858 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 120827 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 120827 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 166591 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 166591 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 141201 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 141201 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 166156 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 166156 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 213804 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 120790 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 120790 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 140369 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 140369 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 120821 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 120821 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 212451 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 212451 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 75158 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 75158 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 166281 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 166281 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 75022 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 75022 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 66579 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 66579 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 84258 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 84258 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 78141 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 78141 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 120823 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 120823 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 124676 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 124676 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 6182 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 6182 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 120832 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 120832 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 140788 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 140788 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 5955 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 5955 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 140354 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 140354 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 139957 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 139957 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 76397 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 76397 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 75825 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 75825 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 139189 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 139189 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 139231 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 139231 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 166468 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 166468 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 168657 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 168657 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 76074 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 76074 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 75634 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 75634 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 66779 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 66779 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 75665 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 75665 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 212324 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 172388 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 172388 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 172388 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 172388 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 174015 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 174015 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 174015 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 174015 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 68702 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 68702 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 83116 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 83116 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 155016 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 155016 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 154793 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 154793 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 94817 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 94817 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 97386 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 97386 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 89481 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 89481 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 158833 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 158833 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 97200 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 97200 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 154719 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 154719 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 88278 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 88278 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 154600 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 154600 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 154719 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 154719 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 97352 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 97352 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 97200 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 97200 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 97120 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 97120 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 97154 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 97154 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 68694 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 68694 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 97149 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 97149 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 154793 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 154793 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 94817 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 94817 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 155063 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 155063 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 155016 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 155016 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 1757 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 2204 19 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 2204 19 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 2204 19 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 4017 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21402696
121879 2204 19 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 2204 19 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 2204 19 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 1757 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10628755
1099 1757 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
121879 2204 19 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 2204 19 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 2204 19 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 1764 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
4345065 1764 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
1093 1764 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
4345065 1764 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
178024 1940 30 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 1940 30 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 1940 30 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 1940 30 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 1940 30 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 1940 30 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 1757 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12907757
1099 1757 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21402696
5866 3567 3 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 3567 3 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 3567 3 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 2299 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 218 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 218 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 218 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 2093 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 2093 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 1844 6 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 1844 6 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 1844 6 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 3567 3 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 3567 3 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 3567 3 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 1844 6 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 1844 6 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 1844 6 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




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
178024 1940 30 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 1940 30 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 1940 30 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 10218 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 10218 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 91401 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 91401 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 10218 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 10218 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 85575 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 85575 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 138745 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 138745 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 85575 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 85575 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 138745 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 138745 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 182435 3 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 182435 3 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 10212 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 10212 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 10212 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 10212 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 77525 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 77525 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 180941 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 180941 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 108812 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 108812 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 77525 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 77525 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 167591 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 167591 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 167591 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 167591 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 100755 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 100755 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 10209 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 10209 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 100619 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 100619 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 100619 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 178804 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 178804 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 178804 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 178804 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 187784 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 187784 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 97818 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 97818 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 97818 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 97818 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 97818 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 97818 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 162219 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 162219 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 162219 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 162219 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 162219 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 162219 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 139590 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 139590 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 139590 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 139590 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 10211 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 10211 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 100755 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 100755 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 10208 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 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 10208 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 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 10208 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 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 10208 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 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 10211 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 10211 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 10213 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 10213 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 10213 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 10213 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 187603 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 187603 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 187603 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 187603 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 10311 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 10311 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 77391 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 77391 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 98792 12 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 98792 12 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 140679 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 140679 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 207185 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 9635 27 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 9635 27 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 10311 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 10311 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 77391 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 77391 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 98792 12 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 98792 12 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 140679 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 140679 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 207185 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 76908 0 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 76908 0 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 76908 0 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 76908 0 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 10206 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 10206 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 10206 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 10206 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 10217 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 10217 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 137661 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 137661 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 139006 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 139006 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 168718 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 168718 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 10217 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 10217 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 137661 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 137661 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 139006 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 139006 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 168718 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 168718 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 10207 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 10207 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 10207 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 10207 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 101721 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 101721 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 183029 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 183029 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 10216 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 10216 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 10216 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 10216 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 10215 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 10215 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 100771 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 100771 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 10215 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 10215 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 100771 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 100771 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 140805 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 140805 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 140805 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 140805 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 209818 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 10210 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 10210 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 10214 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 10214 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 10210 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 10210 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 10214 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 10214 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 62586 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 62586 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 112944 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 112944 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 212362 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 192813 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 192813 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 192813 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 207750 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 108784 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 108784 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 212344 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 112948 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 112948 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 207748 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 140804 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 140804 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 108083 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 108083 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 121074 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 121074 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 112973 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 112973 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 63536 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 63536 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 211583 15 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 211583 15 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 212344 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 108786 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 108786 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 121495 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 121495 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 112949 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 112949 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 96486 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 96486 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 96486 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 96486 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 165484 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 165484 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 121488 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 121488 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 165484 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 165484 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 112947 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 112947 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 112972 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 112972 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 112946 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 112946 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 212344 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 121484 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 121484 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 112983 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 112983 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 1940 30 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 1940 30 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 1940 30 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 76991 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 76991 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 138006 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 138006 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 188136 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 188136 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 188136 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 121487 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 121487 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 112976 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 112976 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 121495 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 121495 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 112955 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 112955 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 78750 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 78750 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 1940 30 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 1940 30 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 1940 30 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 112954 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 112954 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 112974 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 112974 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 124672 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 124672 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 96486 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 96486 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 91118 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 91118 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 112971 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 112971 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 1940 30 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 1940 30 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 1940 30 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 112952 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 112952 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 112951 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 112951 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 120820 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 120820 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 154250 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 154250 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 211983 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 1940 30 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 1940 30 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 1940 30 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 211278 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 112950 13 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 112950 13 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 75635 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 75635 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 213921 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 145123 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 145123 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 108834 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 108834 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 112982 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 112982 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 207747 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 121073 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 121073 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 121484 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 121484 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 207749 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 75158 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 75158 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 93967 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 93967 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 108789 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 108789 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 108790 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 108790 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 98972 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 98972 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 3567 3 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 3567 3 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 3567 3 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 75640 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 75640 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 124673 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 124673 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 112942 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 112942 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 112956 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 112956 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 124677 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 124677 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 108785 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 108785 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 75654 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 75654 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 76414 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 76414 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 108807 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 108807 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 108826 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 108826 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 123039 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 123039 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 108812 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 108812 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 108822 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 108822 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 154105 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 154105 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 108808 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 108808 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 93750 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 93750 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 94184 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 94184 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 1940 30 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 1940 30 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 1940 30 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 91582 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 91582 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 76790 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 76790 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 120838 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 120838 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 84297 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 84297 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 177553 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 177553 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 161735 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 161735 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 161965 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 161965 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 136711 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 136711 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 161716 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 161716 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 177081 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 177081 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 178951 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 178951 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 75521 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 75521 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 207746 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 177553 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 177553 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 93751 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 93751 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 63748 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 63748 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 161735 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 161735 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 75519 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 75519 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 154104 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 154104 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 141268 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 141268 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 141268 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 141268 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 5877 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 5877 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 91843 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 91843 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 129933 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 129933 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 207752 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 121064 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 121064 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 93749 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 93749 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 84512 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 84512 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 137151 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 137151 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 108836 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 108836 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 137151 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 137151 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 146406 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 146406 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 76287 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 76287 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 75672 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 75672 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 121495 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 121495 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 154140 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 154140 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 65831 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 65831 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 83918 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 83918 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 75176 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 75176 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 121067 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 121067 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 7845 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 7845 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 154141 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 154141 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 81189 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 81189 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 91332 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 91332 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 162170 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 162170 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 64085 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 64085 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 81194 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 81194 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 208176 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 136512 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 136512 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 108791 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 108791 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 108827 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 108827 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 136512 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 136512 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 212349 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 126246 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 126246 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 91839 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 91839 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 161729 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 161729 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 162112 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 162112 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 162143 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 162143 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 162226 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 162226 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 159765 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 159765 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 166177 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 166177 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 84713 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 84713 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 108817 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 108817 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 108823 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 108823 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 75525 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 75525 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 84258 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 84258 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 112962 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 112962 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
44582528 192813 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
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/jm8014519
91935097 192813 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
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/jm8014519
CHEMBL525994 192813 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
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/jm8014519
CHEMBL499371 212324 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 81204 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 81204 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 81204 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 81204 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 121518 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 121518 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 84258 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 84258 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 66779 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 66779 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 98696 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 98696 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 120822 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 120822 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 75157 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 75157 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 2420 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 2420 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 2420 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 2420 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 84513 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 84513 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 210019 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 161936 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 161936 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 210019 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 78094 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 78094 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 161936 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 161936 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 11170 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 11170 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 11170 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 5695 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 5695 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 78748 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 78748 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 75204 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 75204 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 112939 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 112939 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 5552 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 5552 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 212451 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 212451 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 162226 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 162226 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 211894 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 62669 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 62669 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 62669 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 62669 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 120825 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 120825 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 136670 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 136670 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 161239 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 161239 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 169466 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 169466 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 62669 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 62669 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 177593 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 177593 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 94120 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 94120 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 123340 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 123340 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 108652 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 108652 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 66742 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 66742 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 64873 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 64873 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 148234 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 148234 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 81207 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 81207 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 81207 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 81207 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 147779 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 147779 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 5703 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 5703 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 65855 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 65855 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 154401 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 154401 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 136699 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 136699 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 75522 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 75522 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 161729 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 161729 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 162112 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 162112 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 162143 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 162143 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 5732 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 5732 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 177339 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 177339 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 154367 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 154367 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 136585 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 136585 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 136669 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 136669 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 141408 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 141408 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 154878 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 154878 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 121064 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 121064 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 12689 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 12689 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 12689 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 84273 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 84273 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 123862 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 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 123862 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 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 188276 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 188276 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 188276 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 188276 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 136196 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 136196 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 108818 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 108818 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 136196 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 136196 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 112979 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 112979 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 176724 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 176724 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 63313 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 63313 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 91838 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 91838 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 176724 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 176724 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 177007 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 177007 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 177339 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 177339 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 162174 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 162174 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 1578 41 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 1578 41 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 1578 41 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 66579 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 66579 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 121062 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 121062 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 120790 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 120790 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 83916 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 83916 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 137609 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 137609 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 167813 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 167813 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 6463 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 6463 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 137871 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 137871 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 147636 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 147636 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 81210 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 81210 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 81210 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 81210 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 12985 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 12985 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 12985 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 64129 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 64129 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 108787 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 108787 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 91583 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 91583 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 162174 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 162174 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 77531 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 77531 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 75906 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 75906 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 5751 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 5751 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 98696 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 98696 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 124679 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 124679 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 97898 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 97898 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 93752 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 93752 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 75029 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 75029 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 65772 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 65772 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 109261 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 109261 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 5706 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 5706 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 174462 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 174462 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 81198 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 81198 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 66000 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 66000 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 97898 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 97898 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 173738 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 173738 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 81202 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 81202 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 5632 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 5632 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 67003 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 67003 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 77359 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 77359 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 177007 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 177007 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 167835 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 167835 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 121065 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 121065 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 136116 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 136116 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 5687 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 5687 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 149958 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 149958 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 154852 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 154852 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 166216 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 166216 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 161349 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 161349 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 90528 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 90528 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 98693 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 98693 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 66008 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 66008 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 1578 41 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 1578 41 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 1578 41 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 137353 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 137353 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 137353 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 137353 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 145620 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 145620 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 152523 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 152523 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 138768 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 138768 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 154281 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 154281 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 121066 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 121066 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 161540 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 161540 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 97936 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 97936 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 63691 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 63691 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 75046 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 75046 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 161707 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 161707 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 161506 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 161506 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 161735 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 161735 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 78754 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 78754 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 165373 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 165373 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 165373 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 165373 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 76391 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 76391 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 177368 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 177368 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 9635 27 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 9635 27 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 108832 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 108832 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 78742 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 78742 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 119836 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 119836 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 176618 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 176618 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 62176 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 62176 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 140029 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 140029 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 123514 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 123514 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 84316 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 84316 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 81206 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 81206 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 81206 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 81206 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 75513 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 75513 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 161506 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 161506 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 161540 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 161540 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 161707 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 161707 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 161735 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 161735 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 143510 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 143510 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 120828 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 120828 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 120832 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 120832 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 1940 30 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 1940 30 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 1940 30 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 75684 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 75684 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 5753 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 5753 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 121485 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 121485 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 3567 3 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 3567 3 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 3567 3 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 212344 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 212344 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 76353 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 76353 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 140788 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 140788 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 108824 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 108824 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 139957 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 139957 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 75676 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 75676 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 75632 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 75632 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 75634 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 75634 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 112978 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 112978 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 98515 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 98515 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 13857 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 13857 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 13857 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 108828 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 108828 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 168440 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 168440 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 76479 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 76479 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 121069 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 121069 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 75531 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 75531 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 11929 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 11929 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 11929 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 64900 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 64900 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 141079 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 141079 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 75022 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 75022 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 75615 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 75615 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 177368 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 177368 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 5752 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 5752 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 162170 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 162170 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 112960 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 112960 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 212662 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 177641 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 177641 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 75514 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 75514 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 97797 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 97797 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 75514 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 75514 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 137489 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 137489 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 9635 27 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 9635 27 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 98763 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 98763 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 2420 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 2420 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 2420 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 2420 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 120821 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 120821 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 154442 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 154442 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 136668 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 136668 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 137069 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 137069 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 64542 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 64542 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 141280 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 141280 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 79314 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 79314 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 68465 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 68465 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 108815 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 108815 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 146654 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 146654 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 112967 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 112967 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 75516 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 75516 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 121067 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 121067 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 78751 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 78751 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 120834 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 120834 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 120837 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 120837 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 84252 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 84252 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 162474 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 162474 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 5665 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 5665 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 75827 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 75827 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 161951 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 161951 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 76389 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 76389 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 177334 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 177334 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 123869 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 123869 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 179629 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 179629 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 75527 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 75527 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 97990 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 97990 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 120824 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 120824 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
CHEMBL500468 212344 0 None - 1 Human 6.6 pIC50 = 6.6 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 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/jm8014519
CHEMBL3586019 210054 4 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 121072 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 121072 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 177334 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 177334 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 161951 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 161951 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 162474 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 162474 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 91156 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 91156 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 121494 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 121494 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 121063 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 121063 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 5684 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 5684 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 11157 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 11157 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 11157 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 108837 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 108837 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 112965 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 112965 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 188250 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 188250 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 188250 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 188250 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 154138 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 154138 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 65237 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 65237 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 176736 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 176736 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 5596 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 5596 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 146774 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 146774 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 76700 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 76700 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 81205 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 81205 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 81205 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 81205 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 75905 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 75905 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 136700 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 136700 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 78744 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 78744 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 5741 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 5741 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 121485 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 121485 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 2204 19 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 2204 19 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 2204 19 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 208176 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 162179 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 162179 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 66677 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 66677 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 161320 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 161320 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 78749 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 78749 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 162037 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 162037 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 176761 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 176761 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 97990 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 97990 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 75644 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 75644 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 75529 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 75529 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 75515 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 75515 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 124675 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 124675 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 120827 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 120827 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 154137 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 154137 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 121494 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 121494 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 124678 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 124678 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 212364 19 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 124674 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 124674 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 124676 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 124676 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 120831 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 120831 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 76397 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 76397 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 206726 34 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 76319 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 76319 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 112977 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 112977 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 1844 6 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 1844 6 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 1844 6 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 176915 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 176915 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 161751 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 161751 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 5747 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 5747 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 91845 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 91845 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 1940 30 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 1940 30 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 1940 30 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 161351 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 161351 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 135761 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 135761 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 76182 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 76182 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 9635 27 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 9635 27 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 138406 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 138406 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 176761 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 176761 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 162037 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 162037 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 162384 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 162384 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 84007 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 84007 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 140315 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 140315 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 140315 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 140315 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 5878 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 5878 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 161514 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 161514 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 162179 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 162179 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 75848 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 75848 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 126246 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 126246 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 1940 30 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 1940 30 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 1940 30 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 154358 18 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 154358 18 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 108809 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 108809 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 145896 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 145896 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 151946 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 151946 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 154358 18 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 154358 18 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 121488 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 121488 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 75532 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 75532 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 207580 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 207580 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 74716 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 74716 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 154106 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 154106 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 136712 0 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 136712 0 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 112980 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 112980 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 98693 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 98693 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 124538 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 124538 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 154475 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 154475 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 12815 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 12815 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 12815 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 12984 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 12984 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 12984 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 62270 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 62270 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 161514 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 161514 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 161406 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 161406 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 162384 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 162384 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 78746 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 78746 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 64245 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 64245 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 121070 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 121070 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 12949 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 12949 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 12949 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 167280 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 167280 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 167335 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 167335 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 75533 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 75533 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 121065 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 121065 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 121494 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 121494 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 11946 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 11946 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 11946 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 81192 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 81192 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 176549 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 176549 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 79807 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 79807 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 167775 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 167775 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 75438 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 75438 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 91842 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 91842 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 108814 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 108814 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 64283 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 64283 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 81208 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 81208 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 81208 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 81208 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 90218 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 90218 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 115698 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 115698 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 147781 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 147781 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 140686 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 140686 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 120826 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 120826 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 68465 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 68465 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 81191 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 81191 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 126652 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 126652 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 66337 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 66337 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 126304 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 126304 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 98763 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 98763 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 192798 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 192798 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 192798 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 192798 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 176549 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 176549 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 177649 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 177649 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 121068 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 121068 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 98972 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 98972 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 138290 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 138290 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 97797 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 97797 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 162453 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 162453 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 120830 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 120830 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 176915 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 176915 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 161751 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 161751 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 138712 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 138712 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 131470 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 131470 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 75148 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 75148 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 121074 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 121074 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 76371 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 76371 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 112943 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 112943 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 64511 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 64511 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 75528 14 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 75528 14 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 177515 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 177515 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 108835 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 108835 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 108821 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 108821 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 84283 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 84283 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 121061 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 121061 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 108811 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 108811 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 64284 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 64284 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 109844 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 109844 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 75523 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 75523 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 160767 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 160767 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 177649 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 177649 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 136709 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 136709 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 62584 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 62584 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 63132 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 63132 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 121072 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 121072 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 120835 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 120835 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 96503 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 96503 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
44582531 188136 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
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/jm8014519
91935100 188136 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
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/jm8014519
CHEMBL504776 188136 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
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/jm8014519
59446148 174477 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 174477 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 5778 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 5778 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 74072 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 74072 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 162453 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 162453 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 5555 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 5555 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 136684 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 136684 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 108810 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 108810 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 151464 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 151464 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 112964 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 112964 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 98515 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 98515 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 84363 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 84363 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 75520 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 75520 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 6274 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 6274 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 154835 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 154835 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 94215 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 94215 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 154879 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 154879 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 140720 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 140720 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 81188 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 81188 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 81188 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 81188 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 7966 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 7966 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 81195 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 81195 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 5746 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 5746 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 97936 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 97936 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 177124 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 177124 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 177076 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 177076 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 174128 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 174128 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 81200 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 81200 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 145550 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 145550 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 168657 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 168657 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 121069 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 121069 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 140974 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 140974 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 121073 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 121073 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 121484 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 121484 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 84375 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 84375 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 112963 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 112963 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 5664 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 5664 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 12730 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 12730 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 12730 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 207751 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 168743 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 168743 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 93940 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 93940 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 162165 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 162165 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 151466 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 151466 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 96619 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 96619 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 108820 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 108820 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 176807 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 176807 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 176807 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 176807 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 177515 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 177515 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 108819 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 108819 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 112945 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 112945 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 180458 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 180458 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 76164 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 76164 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 121071 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 121071 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 75621 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 75621 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 121495 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 121495 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 140354 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 140354 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 94309 1 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 94309 1 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 94309 1 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 94309 1 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 121488 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 121488 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 108825 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 108825 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 76372 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 76372 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 121487 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 121487 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 75665 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 75665 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 162165 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 162165 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 136029 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 136029 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 108831 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 108831 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 109174 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 109174 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 177072 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 177072 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 177076 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 177076 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 161763 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 161763 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 162241 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 162241 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 162256 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 162256 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 177072 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 177072 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 154476 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 154476 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 81186 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 81186 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 92834 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 92834 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 108833 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 108833 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 84367 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 84367 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 177303 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 177303 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 162256 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 162256 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 166385 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 166385 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 146405 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 146405 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 213804 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 212213 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 212213 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 98055 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 98055 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 91121 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 91121 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 212181 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 81193 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 81193 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 172405 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 172405 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 211538 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 135760 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 135760 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 165737 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 165737 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 62175 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 62175 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 62616 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 62616 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 121066 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 121066 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 212200 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 161763 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 161763 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 84422 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 84422 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 135854 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 135854 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 135854 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 135854 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 145483 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 145483 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 162241 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 162241 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 121071 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 121071 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 5784 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 5784 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 81187 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 81187 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 81187 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 81187 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 65871 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 65871 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 75216 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 75216 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 165709 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 165709 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 66736 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 66736 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 154441 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 154441 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 212379 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 161202 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 161202 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 108788 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 108788 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 75526 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 75526 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 91373 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 91373 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 98055 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 98055 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 11159 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 11159 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 11159 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 62663 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 62663 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 120833 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 120833 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 136503 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 136503 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 136503 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 136503 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 136503 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 136503 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 136503 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 136503 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 152522 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 152522 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 62663 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 62663 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 74715 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 74715 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 165273 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 165273 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 206726 34 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 108813 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 108813 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 140478 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 140478 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 115697 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 115697 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 78747 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 78747 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 121494 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 121494 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 112981 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 112981 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 121068 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 121068 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 77000 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 77000 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 154249 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 154249 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 141201 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 141201 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 108829 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 108829 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 212212 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 2204 19 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 2204 19 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 2204 19 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 168987 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 168987 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 98398 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 98398 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 206726 34 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 156700 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 156700 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 96593 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 96593 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 75828 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 75828 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 141201 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 141201 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 207314 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 5785 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 5785 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 146486 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 146486 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 2204 19 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 2204 19 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 2204 19 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 176506 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 176506 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 161525 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 161525 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 162392 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 162392 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 76057 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 76057 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 84473 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 84473 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 136667 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 136667 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 120836 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 120836 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 112940 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 112940 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 76074 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 76074 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 114880 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 114880 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 148485 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 148485 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 137610 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 137610 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 78363 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 78363 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 143749 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 143749 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 12911 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 12911 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 12911 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 94080 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 94080 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 76981 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 76981 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 176506 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 176506 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 5783 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 5783 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 162392 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 162392 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 5707 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 5707 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 121520 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 121520 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 94210 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 94210 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 98212 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 98212 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 74651 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 74651 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 126246 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 126246 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 208830 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 121070 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 121070 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 112984 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 112984 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 108806 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 108806 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 74651 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 74651 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 138007 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 138007 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 108816 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 108816 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 75825 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 75825 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 161174 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 161174 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 78752 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 78752 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 79491 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 79491 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 210022 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 210022 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 93753 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 93753 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 83900 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 83900 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 76388 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 76388 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 161525 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 161525 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 62749 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 62749 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 79806 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 79806 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 121062 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 121062 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 81209 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 81209 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 81209 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 81209 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 172467 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 172467 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 81201 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 81201 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 66736 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 66736 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 84305 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 84305 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 81197 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 81197 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 64252 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 64252 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 90812 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 90812 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 161321 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 161321 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 112961 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 112961 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 64092 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 64092 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 5740 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 5740 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 177056 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 177056 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 210020 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 207579 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 207579 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 137287 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 137287 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 210020 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 176928 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 176928 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 177056 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 177056 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 162445 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 162445 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 160784 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 160784 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 160784 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 177087 2 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 177087 2 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 94239 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 94239 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 77563 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 77563 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 5733 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 5733 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 11927 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 11927 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 11927 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 124680 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 124680 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 112941 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 112941 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 112938 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 112938 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 112953 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 112953 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 154139 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 154139 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 136977 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 136977 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
CHEMBL501253 212362 0 None - 0 Human 7.1 pIC50 = 7.1 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 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/jm8014519
122182045 121486 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 121486 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 94546 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 94546 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 66935 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 66935 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 167790 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 167790 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 81203 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 81203 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 81203 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 81203 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 81190 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 81190 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 81190 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 81190 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 154584 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 154584 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 122723 33 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 122723 33 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 9197 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 9197 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 11917 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 11917 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 11917 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 168148 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 168148 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 75199 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 75199 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 112966 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 112966 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 121828 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 121828 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 176928 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 176928 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 121061 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 121061 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 120823 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 120823 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 84572 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 84572 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 5633 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 5633 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 136110 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 136110 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 172252 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 172252 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 81199 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 81199 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 81196 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 81196 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 75518 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 75518 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 75524 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 75524 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 168081 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 168081 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 65807 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 65807 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
CHEMBL526723 213921 0 None - 0 Human 6.1 pIC50 = 6.1 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 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/jm8014519
CHEMBL335799 209818 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 214062 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 161350 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 161350 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 162445 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 162445 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 123948 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 123948 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 78743 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 78743 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 78743 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 78743 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 122721 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 122721 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 121486 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 121486 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 75581 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 75581 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 121487 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 121487 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 91568 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 91568 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 211052 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 74651 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 74651 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 212344 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 74664 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 74664 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 121488 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 121488 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 75530 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 75530 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 121063 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 121063 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 123336 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 123336 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 121654 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 121654 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 161716 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 161716 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 96592 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 96592 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 84272 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 84272 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 78753 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 78753 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 76796 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 76796 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 12735 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 12735 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 12735 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 1049 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 1049 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 1049 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 212317 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 5683 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 5683 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 210021 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 210021 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 161965 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 161965 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 108830 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 108830 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 62247 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 62247 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 1940 30 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 1940 30 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 1940 30 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 70932 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 70932 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 70933 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 70933 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 70949 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 70949 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 70940 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 70940 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 68694 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 68694 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 68695 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 68695 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 68708 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 68708 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 68710 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 68710 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 68711 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 68711 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 68721 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 68721 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 68726 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 68726 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 142294 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 142294 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 142605 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 142605 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 142973 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 142973 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 143518 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 143518 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 143836 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 143836 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 144034 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 144034 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 144081 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 144081 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 144399 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 144399 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 144853 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 144853 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 144914 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 144914 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 145041 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 145041 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 145400 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 145400 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 145404 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 145404 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 145658 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 145658 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 145914 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 145914 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 146844 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 146844 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 147477 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 147477 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 147639 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 147639 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 148155 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 148155 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 148254 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 148254 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 150067 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 150067 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 150099 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 150099 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 150662 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 150662 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 150810 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 150810 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 151753 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 151753 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 152234 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 152234 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 153502 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 153502 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 70929 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 70929 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 70930 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 70930 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 70938 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 70938 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 1940 30 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 1940 30 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 1940 30 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 70946 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 70946 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 70948 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 70948 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 70939 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 70939 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 68702 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 68702 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 112889 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 112889 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 68702 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 68702 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 68714 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 68714 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 70936 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 70936 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 180643 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 180643 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 110032 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 110032 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 70942 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 70942 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 180535 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 180535 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 70944 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 70944 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 182440 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 182440 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 212344 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 124675 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 124675 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 68724 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 68724 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 70931 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 70931 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 179146 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 179146 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 172388 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 172388 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 211583 15 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 211583 15 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 179900 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 179900 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 70945 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 70945 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 70925 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 70925 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 70947 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 70947 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 68671 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 68671 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 68693 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 68693 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 68701 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 68701 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 68709 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 68709 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 68719 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 68719 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 68720 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 68720 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 68722 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 68722 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 68727 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 68727 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 141841 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 141841 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 141864 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 141864 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 141936 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 141936 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 141975 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 141975 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 142011 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 142011 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 142070 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 142070 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 142344 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 142344 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 142367 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 142367 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 142704 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 142704 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 142819 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 142819 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 142820 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 142820 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 142921 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 142921 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 143162 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 143162 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 143479 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 143479 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 144128 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 144128 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 144280 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 144280 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 144330 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 144330 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 144331 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 144331 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 144627 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 144627 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 144651 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 144651 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 144754 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 144754 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 144793 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 144793 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 144842 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 144842 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 145227 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 145227 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 145325 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 145325 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 145529 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 145529 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 145840 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 145840 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 145871 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 145871 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 146021 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 146021 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 146120 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 146120 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 146196 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 146196 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 146257 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 146257 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 146461 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 146461 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 146585 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 146585 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 146880 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 146880 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 147219 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 147219 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 147222 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 147222 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 147482 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 147482 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 147822 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 147822 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 147921 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 147921 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 147942 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 147942 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 147988 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 147988 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 148011 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 148011 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 148248 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 148248 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 148487 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 148487 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 148558 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 148558 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 148572 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 148572 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 148594 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 148594 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 148917 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 148917 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 148957 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 148957 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 149231 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 149231 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 149253 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 149253 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 149559 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 149559 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 149617 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 149617 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 149741 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 149741 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 149753 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 149753 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 149798 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 149798 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 149802 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 149802 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 150480 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 150480 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 150482 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 150482 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 150560 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 150560 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 150847 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 150847 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 151114 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 151114 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 151583 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 151583 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 151624 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 151624 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 151767 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 151767 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 151910 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 151910 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 152000 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 152000 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 152188 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 152188 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 152366 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 152366 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 152527 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 152527 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 152570 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 152570 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 152634 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 152634 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 152785 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 152785 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 152925 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 152925 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 152989 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 152989 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 153138 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 153138 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 153324 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 153324 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 153423 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 153423 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 153520 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 153520 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 153728 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 153728 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 153766 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 153766 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 124673 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 124673 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 179156 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 179156 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 181553 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 181553 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 91853 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 91853 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 111243 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 111243 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 68673 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 68673 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 68675 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 68675 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 68676 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 68676 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 68677 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 68677 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 68698 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 68698 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 68715 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 68715 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 68717 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 68717 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 68718 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 68718 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 83116 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 83116 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 141863 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 141863 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 142103 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 142103 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 142188 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 142188 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 142222 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 142222 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 142387 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 142387 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 142809 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 142809 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 142987 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 142987 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 143136 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 143136 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 143145 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 143145 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 143199 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 143199 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 143462 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 143462 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 143547 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 143547 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 143583 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 143583 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 143606 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 143606 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 143800 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 143800 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 143859 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 143859 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 143952 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 143952 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 143978 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 143978 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 144032 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 144032 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 144116 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 144116 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 144168 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 144168 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 144395 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 144395 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 144438 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 144438 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 144605 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 144605 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 144677 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 144677 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 144810 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 144810 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 144869 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 144869 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 144927 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 144927 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 144940 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 144940 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 145203 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 145203 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 145401 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 145401 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 145806 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 145806 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 146087 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 146087 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 146132 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 146132 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 146162 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 146162 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 146692 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 146692 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 146854 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 146854 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 147021 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 147021 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 147103 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 147103 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 147132 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 147132 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 147441 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 147441 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 147453 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 147453 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 147544 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 147544 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 147602 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 147602 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 147633 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 147633 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 147786 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 147786 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 147833 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 147833 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 147947 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 147947 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 148073 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 148073 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 148167 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 148167 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 148270 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 148270 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 148491 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 148491 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 148494 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 148494 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 148498 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 148498 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 148502 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 148502 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 148583 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 148583 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 148781 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 148781 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 148903 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 148903 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 148914 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 148914 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 149166 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 149166 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 149285 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 149285 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 149325 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 149325 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 149406 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 149406 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 149434 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 149434 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 149579 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 149579 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 149608 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 149608 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 149624 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 149624 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 149919 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 149919 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 149956 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 149956 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 149994 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 149994 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 150124 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 150124 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 150505 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 150505 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 150518 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 150518 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 150819 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 150819 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 150870 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 150870 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 150878 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 150878 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 151016 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 151016 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 151073 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 151073 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 151291 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 151291 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 151294 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 151294 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 151324 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 151324 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 151393 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 151393 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 151547 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 151547 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 151838 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 151838 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 151862 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 151862 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 151870 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 151870 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 151871 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 151871 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 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 548 5 4 5 3.4 CCCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3970856 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 548 5 4 5 3.4 CCCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134154612 151979 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 151979 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 152047 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 152047 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 152212 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 152212 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 152293 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 152293 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 152674 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 152674 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 152678 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 152678 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 152684 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 152684 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 152820 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 152820 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 152846 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 152846 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 152868 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 152868 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 152949 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 152949 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 153032 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 153032 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 153097 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 153097 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 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 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 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 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 153214 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 153214 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 153227 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 153227 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 153618 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 153618 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 153812 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 153812 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 68672 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 68672 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 68674 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 68674 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 143102 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 143102 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 143152 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 143152 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 143401 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 143401 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 143432 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 143432 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 145676 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 145676 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 145713 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 145713 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 145744 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 145744 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 145837 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 145837 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 146106 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 146106 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 146111 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 146111 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 146195 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 146195 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 146950 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 146950 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 147749 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 147749 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 147952 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 147952 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 148104 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 148104 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 149062 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 149062 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 149404 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 149404 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 150486 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 150486 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 150556 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 150556 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 150595 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 150595 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 150818 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 150818 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 151032 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 151032 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 151302 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 151302 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 151515 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 151515 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 151548 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 151548 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 152334 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 152334 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 152339 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 152339 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 152383 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 152383 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 152642 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 152642 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 152666 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 152666 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 153021 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 153021 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 153136 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 153136 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 153165 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 153165 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 153560 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 153560 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 153672 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 153672 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 68704 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 68704 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 147498 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 147498 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 147331 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 147331 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 75522 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 75522 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 139177 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 139177 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 139164 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 139164 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 68674 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 68674 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 91833 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 91833 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 75523 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 75523 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 181653 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 181653 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 67191 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 67191 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 66609 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 66609 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 67019 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 67019 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 68723 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 68723 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 124677 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 124677 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 179298 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 179298 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 111246 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 111246 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 68677 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 68677 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 68672 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 68672 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 81431 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 81431 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 181570 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 181570 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 116692 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 116692 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 168294 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 168294 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 66435 3 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 66435 3 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 68697 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 68697 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 116688 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 116688 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 180401 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 180401 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 180566 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 180566 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 180828 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 180828 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 139189 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 139189 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 123751 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 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 123751 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 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 179616 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 179616 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 67016 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 67016 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 89762 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 89762 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 91846 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 91846 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 116693 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 116693 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 75521 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 75521 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 75525 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 75525 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 75530 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 75530 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 111246 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 111246 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 180637 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 180637 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 182249 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 182249 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 115696 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 115696 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 68706 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 68706 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 91852 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 91852 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 111245 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 111245 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 68715 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 68715 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 75520 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 75520 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 139403 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 139403 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 139442 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 139442 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 89347 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 89347 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 68696 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 68696 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 71258 13 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 71258 13 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 71258 13 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 91830 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 91830 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 111246 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 111246 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 68716 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 68716 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 180501 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 180501 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 116687 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 116687 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 180734 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 180734 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 91835 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 91835 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 75526 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 75526 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 139331 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 139331 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 139413 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 139413 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 182927 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 182927 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 91841 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 91841 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 145748 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 145748 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 147150 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 147150 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 88345 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 88345 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 139084 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 139084 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 9224 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 9224 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 68725 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 68725 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 89600 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 89600 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 144917 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 144917 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 66941 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 66941 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 166936 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 166936 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 70926 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 70926 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 124676 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 124676 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 179258 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 179258 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 139036 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 139036 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 68726 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 68726 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 70935 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 70935 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 170874 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 170874 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 75518 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 75518 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 116694 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 116694 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 89481 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 89481 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 179291 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 179291 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 81489 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 81489 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 66440 4 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 66440 4 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 75529 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 75529 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 68709 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 68709 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 139101 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 139101 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 68718 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 68718 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 75514 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 75514 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 166893 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 166893 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 60853 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 60853 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 207616 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 123276 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 123276 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 139206 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 139206 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 181388 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 181388 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 186320 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 186320 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 89170 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 89170 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 75531 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 75531 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 180809 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 180809 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 179795 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 179795 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 207621 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 146001 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 146001 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 88084 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 88084 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 187469 0 None -69 7 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 187469 0 None -69 7 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 207622 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 81491 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 81491 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 75524 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 75524 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 68693 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 68693 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 91844 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 91844 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 186465 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 186465 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 91834 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 91834 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 212451 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 212451 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 212451 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 212451 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 186253 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 186253 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 116691 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 116691 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 67071 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 67071 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 154135 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 154135 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 75532 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 75532 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 91831 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 91831 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 91840 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 91840 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 116695 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 116695 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 182776 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 182776 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 126310 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 126310 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 81439 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 81439 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 91844 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 91844 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 91844 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 91844 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 88278 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 88278 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 139164 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 139164 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 139169 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 139169 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 139169 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 139169 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 139533 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 139533 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 81438 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 81438 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 179963 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 179963 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 181198 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 181198 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 171750 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 171750 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 70934 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 70934 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 70943 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 70943 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 91850 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 91850 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 70937 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 70937 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 170469 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 170469 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 181467 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 181467 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 174015 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 174015 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 207623 13 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 207623 13 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 91847 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 91847 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 186319 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 186319 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 190862 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 190862 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 139237 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 139237 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 179891 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 179891 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 186241 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 186241 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 181928 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 181928 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 207608 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 89478 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 89478 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 68705 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 68705 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 89477 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 89477 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 88147 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 88147 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 68703 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 68703 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 68707 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 68707 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 207609 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 68699 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 68699 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 179949 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 179949 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 91832 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 91832 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 182805 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 182805 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 68673 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 68673 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 68700 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 68700 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 81426 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 81426 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 4049 19 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 4049 19 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 4049 19 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 139427 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 139427 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 116689 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 116689 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 181448 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 181448 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 68695 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 68695 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 72844 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 72844 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 111242 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 111242 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 68713 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 68713 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 207623 13 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 207623 13 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 68676 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 68676 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 68717 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 68717 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 75514 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 75514 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 75514 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 75514 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 145017 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 145017 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 68701 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 68701 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 154358 18 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 154358 18 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 81497 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 81497 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 198250 35 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 198250 35 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 75516 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 75516 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 88875 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 88875 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 124678 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 124678 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 139231 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 139231 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 96565 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 96565 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 88221 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 88221 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 88985 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 88985 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 116685 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 116685 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 68712 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 68712 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 70950 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 70950 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 9052 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 9052 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 75528 14 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 75528 14 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 166935 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 166935 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 111245 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 111245 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 68698 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 68698 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 89476 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 89476 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 75519 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 75519 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 175091 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 175091 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 68722 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 68722 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 182504 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 182504 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 68727 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 68727 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 68697 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 68697 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 139132 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 139132 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 206726 34 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 68708 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 68708 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 179361 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 179361 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 181732 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 181732 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 182722 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 182722 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 91841 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 91841 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 91841 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 91841 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 68694 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 68694 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 116686 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 116686 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 173377 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 173377 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 70941 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 70941 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 179474 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 179474 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 3016 28 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 3016 28 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 3016 28 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 3016 28 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 3016 28 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 3016 28 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 3016 28 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 3016 28 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 111242 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 111242 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 70927 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 70927 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 91841 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 91841 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 68728 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 68728 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 180769 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 180769 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 139410 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 139410 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 139447 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 139447 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 2204 19 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 2204 19 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 2204 19 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 181797 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 181797 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 145503 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 145503 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 181406 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 181406 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 68675 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 68675 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 68671 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 68671 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 165948 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 165948 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 75527 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 75527 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 111244 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 111244 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 75528 14 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 75528 14 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 68711 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 68711 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 9635 27 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 9635 27 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 68710 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 68710 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 91848 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 91848 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 147650 0 None -1023 7 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 147650 0 None -1023 7 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 68713 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 68713 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 212364 19 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 68720 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 68720 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 88645 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 88645 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 139250 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 139250 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 124674 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 124674 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 81429 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 81429 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 180459 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 180459 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 68719 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 68719 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 88063 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 88063 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 91851 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 91851 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 68670 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 68670 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 67181 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 67181 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 68721 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 68721 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 124672 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 124672 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 139332 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 139332 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 182991 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 182991 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 91849 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 91849 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 91851 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 91851 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 91851 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 91851 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 116690 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 116690 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 180278 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 180278 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 183499 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 183499 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 66483 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 66483 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 182807 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 182807 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 145750 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 145750 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 2420 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 2420 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 2420 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 2420 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 2420 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 2420 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 2420 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 2420 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 1294 0 None - 1 Human 7.4 pKd = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12907757
1093 1764 0 None -12 2 Human 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
1093 1764 0 None -12 2 Human 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
4345065 1764 0 None -12 2 Human 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
4345065 1764 0 None -12 2 Human 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
1100 1578 41 None - 1 Human 7.9 pKd = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11061542
6918297 1578 41 None - 1 Human 7.9 pKd = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11061542
CHEMBL108335 1578 41 None - 1 Human 7.9 pKd = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11061542
1099 1757 0 None - 1 Human 9.0 pKd = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12907757
1099 1757 0 None - 1 Human 9.0 pKd = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
1092 3109 0 None - 1 Rat 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
134715446 3109 0 None - 1 Rat 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
2232 3109 0 None - 1 Rat 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
6918245 3109 0 None - 1 Rat 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
CHEMBL106593 3109 0 None - 1 Rat 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
58438464 3016 28 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 3016 28 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 3016 28 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 3016 28 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 3016 28 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 3016 28 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 3016 28 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 3016 28 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 3016 28 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 3016 28 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 3016 28 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 3016 28 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 3021 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 3021 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 3021 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 3021 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 4049 19 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 4049 19 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 4049 19 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 1364 0 None - 1 Rat 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11314756
1098 1364 0 None - 1 Rat 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14763915
1101 650 0 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15339248
10740 1907 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 1907 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 3109 0 None - 1 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
134715446 3109 0 None - 1 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
2232 3109 0 None - 1 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
6918245 3109 0 None - 1 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
CHEMBL106593 3109 0 None - 1 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
178024 1940 30 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 1940 30 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 1940 30 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 1757 0 None - 1 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11314756
1093 1764 0 None 12 2 Rat 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
4345065 1764 0 None 12 2 Rat 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793