Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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name		 GPCRdb
ID		 Reference
ligand		 Vendors

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 Assay
Type

 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
44570962 183855 None 0 Human Functional pEC50 = 10.3 10.3 - 1
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 183855 None 0 Human Functional pEC50 = 10.3 10.3 - 1
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 162825 None 0 Human Functional pEC50 = 10 10.0 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162825 None 0 Human Functional pEC50 = 10 10.0 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 177655 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177655 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 94497 None 1 Human Functional pEC50 = 9.8 9.8 - 1
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 94497 None 1 Human Functional pEC50 = 9.8 9.8 - 1
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 177221 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177221 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177655 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177655 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 94497 None 1 Human Functional pEC50 = 9.8 9.8 - 1
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 94497 None 1 Human Functional pEC50 = 9.8 9.8 - 1
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 183878 None 0 Human Functional pEC50 = 9.8 9.8 - 1
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 183878 None 0 Human Functional pEC50 = 9.8 9.8 - 1
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 177221 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177221 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 154953 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 154953 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 177398 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177398 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 191096 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 191096 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 95891 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 95891 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 159396 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 159396 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 159410 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 159410 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 177398 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177398 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177804 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177804 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177570 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177570 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177804 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177804 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 183986 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 183986 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 176795 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 176795 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 177570 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177570 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 10325 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 10325 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 10325 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 10325 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 97567 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 97567 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 178103 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178103 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 184047 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 184047 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 89005 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 89005 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 178103 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178103 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 109716 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 109716 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 194854 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 194854 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 1969 None 33 Human Functional pEC50 = 9.4 9.4 -1 3
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 1969 None 33 Human Functional pEC50 = 9.4 9.4 -1 3
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 1969 None 33 Human Functional pEC50 = 9.4 9.4 -1 3
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 177470 None 6 Human Functional pEC50 = 9.4 9.4 1905 4
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177470 None 6 Human Functional pEC50 = 9.4 9.4 1905 4
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177482 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177482 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 96213 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 96213 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 191438 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 191438 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 88963 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 88963 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 1969 None 33 Human Functional pEC50 = 9.4 9.4 -1 3
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 1969 None 33 Human Functional pEC50 = 9.4 9.4 -1 3
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 1969 None 33 Human Functional pEC50 = 9.4 9.4 -1 3
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 97799 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 97799 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 155601 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 155601 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 94989 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 94989 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 177470 None 6 Human Functional pEC50 = 9.4 9.4 1905 4
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177470 None 6 Human Functional pEC50 = 9.4 9.4 1905 4
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177482 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177482 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 166874 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 166874 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 177989 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177989 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 63462 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 63462 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 63640 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 63640 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 63640 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 63640 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 63640 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 63640 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 122816 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 122816 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 122816 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 122816 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 155554 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 155554 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 94434 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 94434 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 177288 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177288 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177989 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177989 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 97984 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 97984 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 183567 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 183567 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 88965 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 88965 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 89010 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 89010 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 155560 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 155560 None 0 Human Functional pEC50 = 9.3 9.3 - 1
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 177288 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177288 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 160558 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 160558 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 95259 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 95259 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 10313 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 10313 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 79158 None 1 Human Functional pEC50 = 9.2 9.2 - 1
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 79158 None 1 Human Functional pEC50 = 9.2 9.2 - 1
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 10313 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 10313 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 155076 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 155076 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 88889 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 88889 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 159458 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 159458 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 131786 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 131786 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 161099 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 161099 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 95018 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 95018 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 63090 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 63090 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 178087 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178087 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 93977 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 93977 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 104558 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 104558 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 139273 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 139273 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 177379 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177379 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178087 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178087 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 98027 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 98027 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 157298 None 2 Human Functional pEC50 = 9.1 9.1 - 1
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 157298 None 2 Human Functional pEC50 = 9.1 9.1 - 1
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 157298 None 2 Human Functional pEC50 = 9.1 9.1 - 1
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 157298 None 2 Human Functional pEC50 = 9.1 9.1 - 1
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 88943 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 88943 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 155330 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 155330 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 104558 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 104558 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 139273 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 139273 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 139765 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 139765 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 178204 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178204 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177379 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177379 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 63454 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 63454 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 179100 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 179100 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 9725 None 33 Human Functional pEC50 = 9.1 9.1 -5 2
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 9725 None 33 Human Functional pEC50 = 9.1 9.1 -5 2
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 96472 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 96472 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 9725 None 33 Human Functional pEC50 = 9.0 9.0 -5 2
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 9725 None 33 Human Functional pEC50 = 9.0 9.0 -5 2
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 178053 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178053 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 10323 None 0 Human Functional pEC50 = 9 9.0 - 1
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 10323 None 0 Human Functional pEC50 = 9 9.0 - 1
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 183015 None 5 Human Functional pEC50 = 9 9.0 - 1
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 183015 None 5 Human Functional pEC50 = 9 9.0 - 1
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 177911 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177911 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178053 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178053 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178201 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178201 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178204 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178204 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 69011 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69011 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69017 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69017 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69034 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69034 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69035 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69035 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69042 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69042 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69051 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69051 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69062 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69062 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69066 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69066 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 71600 None 17 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 71600 None 17 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 71600 None 17 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 142371 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 142371 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 142824 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 142824 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 143135 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 143135 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 143451 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 143451 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 143503 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 143503 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 143692 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 143692 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144136 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144136 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144367 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144367 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144565 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144565 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144861 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144861 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144930 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144930 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145285 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145285 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145324 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145324 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145384 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145384 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145572 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145572 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145758 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145758 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145935 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145935 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 146189 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 146189 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 146371 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 146371 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 146445 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 146445 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 146552 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 146552 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 147116 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 147116 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 147750 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 147750 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 147753 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 147753 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 148012 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 148012 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 148352 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 148352 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 148472 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 148472 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 148784 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 148784 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 149088 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 149088 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 149487 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 149487 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 151012 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 151012 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 151090 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 151090 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 152401 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 152401 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 152718 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 152718 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 190257 None 0 Human Functional pEC50 = 9 9.0 - 1
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 190257 None 0 Human Functional pEC50 = 9 9.0 - 1
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 89738 None 0 Human Functional pEC50 = 9 9.0 - 1
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 89738 None 0 Human Functional pEC50 = 9 9.0 - 1
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 88873 None 0 Human Functional pEC50 = 9 9.0 - 1
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 88873 None 0 Human Functional pEC50 = 9 9.0 - 1
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 88888 None 0 Human Functional pEC50 = 9 9.0 - 1
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 88888 None 0 Human Functional pEC50 = 9 9.0 - 1
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 88917 None 0 Human Functional pEC50 = 9 9.0 - 1
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 88917 None 0 Human Functional pEC50 = 9 9.0 - 1
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 88938 None 0 Human Functional pEC50 = 9 9.0 - 1
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 88938 None 0 Human Functional pEC50 = 9 9.0 - 1
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 161812 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 161812 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 177911 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177911 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178201 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178201 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 10307 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 10307 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 10307 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 10307 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 94962 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 94962 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 155561 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 155561 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 27330 None 0 Rat Functional pEC50 = 8.9 8.9 - 1
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 27330 None 0 Rat Functional pEC50 = 8.9 8.9 - 1
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 98339 None 0 Rat Functional pEC50 = 8.9 8.9 - 1
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 98339 None 0 Rat Functional pEC50 = 8.9 8.9 - 1
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 162691 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162691 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 189835 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 189835 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 88960 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 88960 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 88969 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 88969 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 94933 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 94933 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 96316 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 96316 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 1969 None 33 Human Functional pEC50 = 8.9 8.9 -1 3
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 1969 None 33 Human Functional pEC50 = 8.9 8.9 -1 3
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 1969 None 33 Human Functional pEC50 = 8.9 8.9 -1 3
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 1969 None 33 Rat Functional pEC50 = 8.9 8.9 1 3
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 1969 None 33 Rat Functional pEC50 = 8.9 8.9 1 3
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 1969 None 33 Rat Functional pEC50 = 8.9 8.9 1 3
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 1969 None 33 Human Functional pEC50 = 8.9 8.9 -1 3
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 1969 None 33 Human Functional pEC50 = 8.9 8.9 -1 3
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 1969 None 33 Human Functional pEC50 = 8.9 8.9 -1 3
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 162691 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162691 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 95799 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 95799 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 214113 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 214113 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 63823 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 63823 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 214113 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 180543 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 180543 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 214113 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 214113 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 1969 None 33 Human Functional pEC50 = 8.9 8.9 -1 3
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 1969 None 33 Human Functional pEC50 = 8.9 8.9 -1 3
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 1969 None 33 Human Functional pEC50 = 8.9 8.9 -1 3
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 177296 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177296 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 64302 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 64302 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 64614 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 64614 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 64614 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 64614 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 16371 None 0 Rat Functional pEC50 = 8.8 8.8 - 1
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 16371 None 0 Rat Functional pEC50 = 8.8 8.8 - 1
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 213329 None 18 Human Functional pEC50 = 8.8 8.8 - 1
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 213329 None 18 Human Functional pEC50 = 8.8 8.8 - 1
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 162299 None 0 Human Functional pEC50 = 8.8 8.8 57 2
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162299 None 0 Human Functional pEC50 = 8.8 8.8 57 2
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 205299 None 1 Human Functional pEC50 = 8.8 8.8 - 1
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 205299 None 1 Human Functional pEC50 = 8.8 8.8 - 1
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 177296 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177296 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177487 None 0 Human Functional pEC50 = 8.8 8.8 60 3
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177487 None 0 Human Functional pEC50 = 8.8 8.8 60 3
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 88916 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 88916 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 88919 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 88919 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 88962 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 88962 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 88967 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 88967 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 89013 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 89013 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 191292 None 1 Human Functional pEC50 = 8.8 8.8 - 1
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 191292 None 1 Human Functional pEC50 = 8.8 8.8 - 1
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 96932 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 96932 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 205299 None 1 Human Functional pEC50 = 8.8 8.8 - 1
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 205299 None 1 Human Functional pEC50 = 8.8 8.8 - 1
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 91547 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 91547 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 94990 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 94990 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 94963 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 94963 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 208466 None 38 Rat Functional pEC50 = 8.8 8.8 12 2
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 94875 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 94875 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 96344 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 96344 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 24091 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 24091 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 27485 None 0 Rat Functional pEC50 = 8.7 8.7 - 1
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 27485 None 0 Rat Functional pEC50 = 8.7 8.7 - 1
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 112985 None 0 Rat Functional pEC50 = 8.7 8.7 - 1
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 112985 None 0 Rat Functional pEC50 = 8.7 8.7 - 1
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 24091 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 24091 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 177052 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177052 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 153965 None 9 Human Functional pEC50 = 8.7 8.7 - 1
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 153965 None 9 Human Functional pEC50 = 8.7 8.7 - 1
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 153965 None 9 Human Functional pEC50 = 8.7 8.7 - 1
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 153965 None 9 Human Functional pEC50 = 8.7 8.7 - 1
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 153965 None 9 Human Functional pEC50 = 8.7 8.7 - 1
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 153965 None 9 Human Functional pEC50 = 8.7 8.7 - 1
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 153965 None 9 Human Functional pEC50 = 8.7 8.7 - 1
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 153965 None 9 Human Functional pEC50 = 8.7 8.7 - 1
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 10323 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 10323 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 101223 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 101223 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 177052 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177052 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177333 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177333 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177579 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177579 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 96255 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 96255 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 97585 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 97585 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 183957 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 183957 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 88934 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 88934 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 88942 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 88942 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 88978 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 88978 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 89018 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 89018 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 186766 None 0 Human Functional pEC50 = 8 8.0 - 1
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 186766 None 0 Human Functional pEC50 = 8 8.0 - 1
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 94017 None 0 Human Functional pEC50 = 8 8.0 - 1
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 94017 None 0 Human Functional pEC50 = 8 8.0 - 1
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 162072 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162072 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162774 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162774 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 89905 None 0 Human Functional pEC50 = 8 8.0 - 1
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 89905 None 0 Human Functional pEC50 = 8 8.0 - 1
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 5334 None 0 Human Functional pEC50 = 8 8.0 - 1
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 5334 None 0 Human Functional pEC50 = 8 8.0 - 1
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 10304 None 0 Human Functional pEC50 = 8 8.0 - 1
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 10304 None 0 Human Functional pEC50 = 8 8.0 - 1
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 10322 None 0 Human Functional pEC50 = 8 8.0 - 1
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 10322 None 0 Human Functional pEC50 = 8 8.0 - 1
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 101086 None 0 Human Functional pEC50 = 8 8.0 1 2
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 101086 None 0 Human Functional pEC50 = 8 8.0 1 2
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 101086 None 0 Human Functional pEC50 = 8 8.0 1 2
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 139778 None 0 Human Functional pEC50 = 8 8.0 - 1
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 139778 None 0 Human Functional pEC50 = 8 8.0 - 1
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 177332 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177332 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177628 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177628 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 95379 None 0 Human Functional pEC50 = 8 8.0 - 1
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 95379 None 0 Human Functional pEC50 = 8 8.0 - 1
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 184044 None 0 Human Functional pEC50 = 8 8.0 - 1
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 184044 None 0 Human Functional pEC50 = 8 8.0 - 1
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 208466 None 38 Rat Functional pEC50 = 8 8.0 12 2
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 88878 None 0 Human Functional pEC50 = 8 8.0 - 1
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 88878 None 0 Human Functional pEC50 = 8 8.0 - 1
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 88893 None 0 Human Functional pEC50 = 8 8.0 - 1
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 88893 None 0 Human Functional pEC50 = 8 8.0 - 1
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 88894 None 0 Human Functional pEC50 = 8 8.0 - 1
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 88894 None 0 Human Functional pEC50 = 8 8.0 - 1
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 88912 None 0 Human Functional pEC50 = 8 8.0 - 1
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 88912 None 0 Human Functional pEC50 = 8 8.0 - 1
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 88925 None 0 Human Functional pEC50 = 8 8.0 - 1
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 88925 None 0 Human Functional pEC50 = 8 8.0 - 1
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 88968 None 0 Human Functional pEC50 = 8 8.0 - 1
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 88968 None 0 Human Functional pEC50 = 8 8.0 - 1
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 88981 None 0 Human Functional pEC50 = 8 8.0 - 1
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 88981 None 0 Human Functional pEC50 = 8 8.0 - 1
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 89015 None 0 Human Functional pEC50 = 8 8.0 - 1
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 89015 None 0 Human Functional pEC50 = 8 8.0 - 1
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 89017 None 0 Human Functional pEC50 = 8 8.0 - 1
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 89017 None 0 Human Functional pEC50 = 8 8.0 - 1
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 148117 None 0 Human Functional pEC50 = 8 8.0 - 1
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 148117 None 0 Human Functional pEC50 = 8 8.0 - 1
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 177628 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177628 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 167316 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 167316 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 177332 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177332 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 162940 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162940 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 169380 None 0 Human Functional pEC50 = 7 7.0 - 1
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 169380 None 0 Human Functional pEC50 = 7 7.0 - 1
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 96681 None 0 Human Functional pEC50 = 7 7.0 - 1
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 96681 None 0 Human Functional pEC50 = 7 7.0 - 1
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 97812 None 0 Human Functional pEC50 = 7 7.0 - 1
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 97812 None 0 Human Functional pEC50 = 7 7.0 - 1
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 159333 None 0 Human Functional pEC50 = 7 7.0 - 1
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 159333 None 0 Human Functional pEC50 = 7 7.0 - 1
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 69053 None 0 Human Functional pEC50 = 7 7.0 - 1
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 69053 None 0 Human Functional pEC50 = 7 7.0 - 1
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 69055 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69055 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69058 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69058 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69060 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69060 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69061 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69061 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 142466 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 142466 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 143234 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 143234 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144390 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144390 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144659 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144659 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144969 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144969 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145458 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145458 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 146727 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 146727 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 148451 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 148451 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 148778 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 148778 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 149032 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 149032 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 151010 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 151010 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 151340 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 151340 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 151546 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 151546 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 152077 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 152077 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 152113 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 152113 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 152368 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 152368 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 152823 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 152823 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 153317 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 153317 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 153649 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 153649 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 179382 None 0 Human Functional pEC50 = 7 7.0 -14 2
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 179382 None 0 Human Functional pEC50 = 7 7.0 -14 2
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 214220 None 0 Human Functional pEC50 = 7 7.0 - 1
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 214220 None 0 Human Functional pEC50 = 7 7.0 - 1
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 214220 None 0 Human Functional pEC50 = 7 7.0 - 1
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 214220 None 0 Human Functional pEC50 = 7 7.0 - 1
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 211764 None 0 Human Functional pEC50 = 7 7.0 -33 2
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 211767 None 0 Human Functional pEC50 = 7 7.0 -15 2
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 88899 None 0 Human Functional pEC50 = 7 7.0 - 1
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 88899 None 0 Human Functional pEC50 = 7 7.0 - 1
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 88901 None 0 Human Functional pEC50 = 7 7.0 - 1
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 88901 None 0 Human Functional pEC50 = 7 7.0 - 1
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 88910 None 0 Human Functional pEC50 = 7 7.0 - 1
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 88910 None 0 Human Functional pEC50 = 7 7.0 - 1
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 88911 None 0 Human Functional pEC50 = 7 7.0 - 1
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 88911 None 0 Human Functional pEC50 = 7 7.0 - 1
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 88932 None 0 Human Functional pEC50 = 7 7.0 - 1
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 88932 None 0 Human Functional pEC50 = 7 7.0 - 1
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 88949 None 0 Human Functional pEC50 = 7 7.0 - 1
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 88949 None 0 Human Functional pEC50 = 7 7.0 - 1
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 88953 None 0 Human Functional pEC50 = 7 7.0 - 1
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 88953 None 0 Human Functional pEC50 = 7 7.0 - 1
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 88971 None 0 Human Functional pEC50 = 7 7.0 - 1
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 88971 None 0 Human Functional pEC50 = 7 7.0 - 1
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 89000 None 0 Human Functional pEC50 = 7 7.0 - 1
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 89000 None 0 Human Functional pEC50 = 7 7.0 - 1
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 191340 None 0 Human Functional pEC50 = 6 6.0 - 1
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 191340 None 0 Human Functional pEC50 = 6 6.0 - 1
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 178086 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178086 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 146034 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 146034 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 96336 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 96336 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 178086 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178086 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 88510 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 88510 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 211767 None 0 Human Functional pEC50 = 7.0 7.0 -15 2
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 95769 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 95769 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 137206 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 137206 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 69051 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 69051 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 209366 None 15 Human Functional pEC50 = 8.0 8.0 - 1
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 209366 None 15 Human Functional pEC50 = 8.0 8.0 - 1
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 64312 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 64312 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 89413 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 89413 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 146856 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 146856 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 167258 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 167258 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 209361 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 90029 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 90029 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 91550 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 91550 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 141609 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 141609 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 94675 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 94675 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 64316 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 64316 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 209366 None 15 Human Functional pEC50 = 7.9 7.9 - 1
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 209366 None 15 Human Functional pEC50 = 7.9 7.9 - 1
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 177807 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177807 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 162932 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162932 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 177238 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177238 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177807 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177807 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 88871 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 88871 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 88922 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 88922 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 88954 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 88954 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 88970 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 88970 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 88988 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 88988 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 88995 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 88995 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 89021 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 89021 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 89024 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 89024 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 209364 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 184108 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 184108 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 186835 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 186835 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 194198 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 194198 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 192617 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 192617 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 166748 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 166748 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 177764 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177764 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 209362 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 188366 None 0 Rabbit Functional pEC50 = 6.9 6.9 -5 3
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 188366 None 0 Rabbit Functional pEC50 = 6.9 6.9 -5 3
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 154684 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 154684 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 162047 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162047 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162522 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162522 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162727 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162727 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 177230 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177230 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 96326 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 96326 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 88884 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 88884 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 88892 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 88892 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 177764 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177764 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 184749 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 184749 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 167211 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 167211 None 0 Human Functional pEC50 = 5.9 5.9 - 1
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 162727 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162727 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 112840 None 0 Rat Functional pEC50 = 7.9 7.9 - 1
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 112840 None 0 Rat Functional pEC50 = 7.9 7.9 - 1
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 64583 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 64583 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 209368 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 209364 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 177238 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177238 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177230 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177230 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 69010 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 69010 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 148028 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 148028 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 171034 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 171034 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 162047 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162047 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162522 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162522 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 155330 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 155330 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 69042 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 69042 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 162932 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162932 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 146279 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 146279 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 98268 None 0 Human Functional pEC50 = 7.9 7.9 1 3
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 98268 None 0 Human Functional pEC50 = 7.9 7.9 1 3
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 98268 None 0 Human Functional pEC50 = 7.9 7.9 1 3
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 147017 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 147017 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 98268 None 0 Rat Functional pEC50 = 7.9 7.9 -1 3
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 98268 None 0 Rat Functional pEC50 = 7.9 7.9 -1 3
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 98268 None 0 Rat Functional pEC50 = 7.9 7.9 -1 3
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 98268 None 0 Human Functional pEC50 = 7.9 7.9 1 3
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 98268 None 0 Human Functional pEC50 = 7.9 7.9 1 3
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 98268 None 0 Human Functional pEC50 = 7.9 7.9 1 3
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 169380 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 169380 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 183020 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 183020 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 64348 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 64348 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 147872 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 147872 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 160391 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 160391 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 184226 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 184226 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 186993 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 186993 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 96583 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 96583 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 137221 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 137221 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 186958 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 186958 None 0 Human Functional pEC50 = 4.9 4.9 - 1
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 90957 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 90957 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 89775 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 89775 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 162499 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162499 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 79161 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 79161 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 84934 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 84934 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 181039 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 181039 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 94018 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 94018 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 162499 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162499 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 96918 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 96918 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 155223 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 155223 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 183879 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 183879 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 183953 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 183953 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 88872 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 88872 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 88881 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 88881 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 88883 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 88883 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 88895 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 88895 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 88903 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 88903 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 88915 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 88915 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 88923 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 88923 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 88927 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 88927 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 88984 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 88984 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 89014 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 89014 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 89026 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 89026 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 186982 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 186982 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 155256 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 155256 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 168858 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 168858 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 186872 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 186872 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 162484 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162484 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 88656 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 88656 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 181389 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 181389 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 94400 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 94400 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 162804 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162804 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 163001 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 163001 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 177353 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177353 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 159576 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 159576 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 5710 None 0 Human Functional pEC50 = 6.8 6.8 -39 2
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 5710 None 0 Human Functional pEC50 = 6.8 6.8 -39 2
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 88906 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 88906 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 89027 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 89027 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 155389 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 155389 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 162484 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162484 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 5709 None 0 Human Functional pEC50 = 5.8 5.8 -158 2
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 5709 None 0 Human Functional pEC50 = 5.8 5.8 -158 2
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 154676 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 154676 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 98457 None 0 Rat Functional pEC50 = 7.8 7.8 - 1
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 98457 None 0 Rat Functional pEC50 = 7.8 7.8 - 1
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 96541 None 0 Rat Functional pEC50 = 7.8 7.8 - 1
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 96541 None 0 Rat Functional pEC50 = 7.8 7.8 - 1
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 162767 None 0 Human Functional pEC50 = 7.8 7.8 1 2
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 162767 None 0 Human Functional pEC50 = 7.8 7.8 1 2
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 162767 None 0 Human Functional pEC50 = 7.8 7.8 1 2
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 69037 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 69037 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 172955 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 172955 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 10324 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 10324 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 163001 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 163001 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 209369 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 147681 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 147681 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 177353 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177353 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 209355 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 89909 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 89909 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 89909 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 89909 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 10324 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 10324 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 162767 None 0 Human Functional pEC50 = 7.8 7.8 1 2
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 162767 None 0 Human Functional pEC50 = 7.8 7.8 1 2
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 162767 None 0 Human Functional pEC50 = 7.8 7.8 1 2
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 168383 None 0 Rat Functional pEC50 = 7.8 7.8 - 1
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 168383 None 0 Rat Functional pEC50 = 7.8 7.8 - 1
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 123319 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 123319 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 209365 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 162804 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162804 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 139629 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 139629 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 140118 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 140118 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 202518 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 202518 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 138014 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 138014 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 69046 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 69046 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 174585 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 174585 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 99247 None 17 Rat Functional pEC50 = 7.8 7.8 -5 2
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 99247 None 17 Rat Functional pEC50 = 7.8 7.8 -5 2
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 140118 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 140118 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 202518 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 202518 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 186901 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 186901 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 146014 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 146014 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 209356 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 89509 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 89509 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 166769 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 166769 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 211758 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 162585 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162585 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 97601 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 97601 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 97647 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 97647 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 97833 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 97833 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 30039 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
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 30039 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
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 180529 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 180529 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 161953 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 161953 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 12030 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 12030 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 12030 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 64865 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 64865 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 168311 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 168311 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 94470 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 94470 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 162161 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162161 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162585 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162585 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162722 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162722 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 163022 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 163022 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 97541 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 97541 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 5842 None 0 Human Functional pEC50 = 7.7 7.7 3 2
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 5842 None 0 Human Functional pEC50 = 7.7 7.7 3 2
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 183956 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 183956 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 88875 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 88875 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 88908 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 88908 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 88928 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 88928 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 88939 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 88939 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 88958 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 88958 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 88972 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 88972 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 88977 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 88977 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 88980 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 88980 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 88985 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 88985 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 89002 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 89002 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 89008 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 89008 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 89009 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 89009 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 64864 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 64864 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 167343 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 167343 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 177644 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177644 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 211758 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 191456 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 191456 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 162299 None 0 Human Functional pEC50 = 8.7 8.7 57 2
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162299 None 0 Human Functional pEC50 = 8.7 8.7 57 2
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 10306 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 10306 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 101223 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 101223 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 177487 None 0 Human Functional pEC50 = 8.7 8.7 60 3
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177487 None 0 Human Functional pEC50 = 8.7 8.7 60 3
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 63935 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 63935 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 63935 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 63935 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 17104 None 0 Rat Functional pEC50 = 8.7 8.7 - 1
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 17104 None 0 Rat Functional pEC50 = 8.7 8.7 - 1
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 177579 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177579 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177333 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177333 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 10303 None 1 Human Functional pEC50 = 8.7 8.7 - 1
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 10303 None 1 Human Functional pEC50 = 8.7 8.7 - 1
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 10303 None 1 Human Functional pEC50 = 8.7 8.7 - 1
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 10303 None 1 Human Functional pEC50 = 8.7 8.7 - 1
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 64667 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 64667 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 209353 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 177306 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177306 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 113392 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 113392 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 113392 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 113392 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 79160 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 79160 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 64634 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 64634 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 64872 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 64872 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 92012 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 92012 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 174585 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 174585 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 94498 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 94498 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 162277 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162277 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 10306 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 10306 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 177263 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177263 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177306 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177306 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 97926 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 97926 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 183834 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 183834 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 88914 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 88914 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 88937 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 88937 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 88950 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 88950 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 88964 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 88964 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 89019 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 89019 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 10308 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 10308 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 10308 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 10308 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 168065 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 168065 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 209366 None 15 Human Functional pEC50 = 8.6 8.6 - 1
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 209366 None 15 Human Functional pEC50 = 8.6 8.6 - 1
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 177263 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177263 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 168065 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 168065 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 177940 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177940 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 96219 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 96219 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 98224 None 0 Rat Functional pEC50 = 8.5 8.5 - 1
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 98224 None 0 Rat Functional pEC50 = 8.5 8.5 - 1
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 184747 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 184747 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 187046 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 187046 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 187064 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 187064 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 88647 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 88647 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 139859 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 139859 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 69042 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 69042 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 24060 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
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 24060 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
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 113792 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
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 113792 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
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 123908 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 123908 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 186922 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 186922 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 88490 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 88490 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 186895 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 186895 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 187134 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 187134 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 191347 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 191347 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 97647 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 97647 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 158649 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 158649 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 177644 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177644 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 162161 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162161 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162722 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162722 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 163022 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 163022 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 64455 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 64455 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 64459 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 64459 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 114241 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
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 114241 None 0 Rat Functional pEC50 = 7.7 7.7 - 1
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 179724 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 179724 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 188184 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 188184 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 138136 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 138136 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 166707 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 166707 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 62946 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 62946 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 155137 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 155137 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 188184 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 188184 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 172955 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 172955 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 187159 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 187159 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 190419 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 190419 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 162264 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162264 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162993 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162993 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 158701 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 158701 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 159378 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 159378 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 96949 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 96949 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 69035 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 69035 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 181217 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 181217 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 162155 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162155 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 209366 None 15 Human Functional pEC50 = 6.6 6.6 - 1
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 209366 None 15 Human Functional pEC50 = 6.6 6.6 - 1
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 94554 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 94554 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 155372 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 155372 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 16202 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
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 16202 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
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 209357 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 155256 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 155256 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 155522 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 155522 None 0 Human Functional pEC50 = 5.6 5.6 - 1
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 162713 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162713 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 30483 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
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 30483 None 0 Rat Functional pEC50 = 7.6 7.6 - 1
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 180480 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 180480 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 177269 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177269 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 162311 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162311 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162713 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162713 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162993 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162993 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 177269 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177269 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178032 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178032 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 88879 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 88879 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 88904 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 88904 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 88918 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 88918 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 88931 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 88931 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 88935 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 88935 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 88945 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 88945 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 88947 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 88947 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 88957 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 88957 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 88982 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 88982 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 88989 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 88989 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 178032 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178032 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 188899 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 188899 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 162061 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162061 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162061 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162061 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162155 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162155 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162264 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162264 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162533 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162533 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162734 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162734 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 211763 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 91803 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 91803 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 64296 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 64296 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 132101 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 132101 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 89414 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 89414 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 159748 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 159748 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 69062 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 69062 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 128801 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 128801 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 186767 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 186767 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 162734 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162734 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 211763 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 71600 None 17 Human Functional pEC50 = 7.6 7.6 - 1
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 71600 None 17 Human Functional pEC50 = 7.6 7.6 - 1
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 71600 None 17 Human Functional pEC50 = 7.6 7.6 - 1
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 159235 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 159235 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 89072 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 89072 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 97596 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 97596 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 69066 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 69066 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 63862 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 63862 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 181778 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 181778 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 172955 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 172955 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 162533 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162533 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 79150 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 79150 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 162311 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162311 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 179939 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 179939 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 145548 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 145548 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 71600 None 17 Human Functional pEC50 = 7.5 7.5 - 1
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 71600 None 17 Human Functional pEC50 = 7.5 7.5 - 1
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 71600 None 17 Human Functional pEC50 = 7.5 7.5 - 1
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 121261 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 121261 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 166641 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 166641 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 209366 None 15 Human Functional pEC50 = 7.5 7.5 - 1
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 209366 None 15 Human Functional pEC50 = 7.5 7.5 - 1
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 148603 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 148603 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 166579 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 166579 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 184079 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 184079 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 162277 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162277 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162774 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162774 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 158828 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 158828 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 10321 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 10321 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 77742 None 2 Human Functional pEC50 = 8.5 8.5 - 1
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 77742 None 2 Human Functional pEC50 = 8.5 8.5 - 1
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 99247 None 17 Human Functional pEC50 = 8.5 8.5 5 2
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 99247 None 17 Human Functional pEC50 = 8.5 8.5 5 2
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 141208 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 141208 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 208685 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 96932 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 96932 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 96932 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 96932 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 154174 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 154174 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 15576 None 0 Rat Functional pEC50 = 8.5 8.5 - 1
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 15576 None 0 Rat Functional pEC50 = 8.5 8.5 - 1
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 10321 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 10321 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 77742 None 2 Human Functional pEC50 = 8.5 8.5 - 1
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 77742 None 2 Human Functional pEC50 = 8.5 8.5 - 1
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 99247 None 17 Human Functional pEC50 = 8.5 8.5 5 2
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 99247 None 17 Human Functional pEC50 = 8.5 8.5 5 2
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 141208 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 141208 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 208685 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 177376 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177376 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 96613 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 96613 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 94897 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 94897 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 154765 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 154765 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 177376 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177376 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177940 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177940 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 192559 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 192559 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 88961 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 88961 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 88997 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 88997 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 89023 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 89023 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 89029 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 89029 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 95854 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 95854 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 89740 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 89740 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 209366 None 15 Human Functional pEC50 = 8.5 8.5 - 1
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 209366 None 15 Human Functional pEC50 = 8.5 8.5 - 1
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 63636 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 63636 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 122996 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 122996 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 209366 None 15 Human Functional pEC50 = 8.5 8.5 - 1
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 209366 None 15 Human Functional pEC50 = 8.5 8.5 - 1
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 182829 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 182829 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 89590 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 89590 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 209366 None 15 Human Functional pEC50 = 8.4 8.4 - 1
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 209366 None 15 Human Functional pEC50 = 8.4 8.4 - 1
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 93976 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 93976 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 77259 None 1 Human Functional pEC50 = 8.4 8.4 - 1
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 77259 None 1 Human Functional pEC50 = 8.4 8.4 - 1
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 177421 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177421 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 95265 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 95265 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 155026 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 155026 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 5840 None 0 Human Functional pEC50 = 8.4 8.4 1 2
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 5840 None 0 Human Functional pEC50 = 8.4 8.4 1 2
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 5841 None 0 Human Functional pEC50 = 8.4 8.4 -1 2
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 5841 None 0 Human Functional pEC50 = 8.4 8.4 -1 2
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 191303 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 191303 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 88909 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 88909 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 88948 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 88948 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 88959 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 88959 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 88996 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 88996 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 89011 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 89011 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 89020 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 89020 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 88704 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88704 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 186833 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 186833 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 192552 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 192552 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88771 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88771 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88704 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88704 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88704 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88704 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88771 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88771 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 202091 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 202091 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 202517 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 202517 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 202091 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 202091 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 202517 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 202517 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 95260 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 95260 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 167275 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 167275 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 154952 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 154952 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 162513 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162513 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 183954 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 183954 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 189970 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 189970 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 121261 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 121261 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88874 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88874 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88880 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88880 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88882 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88882 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88913 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88913 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88921 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88921 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88929 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88929 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88940 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88940 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88951 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88951 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88952 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88952 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88973 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88973 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88976 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88976 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88983 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88983 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88990 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 88990 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 89004 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 89004 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 89028 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 89028 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 69056 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 69056 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 178122 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178122 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177648 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177648 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178122 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178122 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 95091 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 95091 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 155091 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 155091 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 183426 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 183426 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 211762 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 177648 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177648 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 89416 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 89416 None 0 Human Functional pEC50 = 5.5 5.5 - 1
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 161890 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 161890 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 94645 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 94645 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 214113 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 95800 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 95800 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 94898 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 94898 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 193068 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 193068 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 211762 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 94876 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 94876 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 89904 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 89904 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 162513 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162513 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 89906 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 89906 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 179734 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 179734 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 15551 None 0 Rat Functional pEC50 = 7.5 7.5 - 1
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 15551 None 0 Rat Functional pEC50 = 7.5 7.5 - 1
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 162283 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162283 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 98663 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 98663 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 69060 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 69060 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 166389 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 166389 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 173947 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 173947 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 97176 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
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 97176 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
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 97217 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
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 97217 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
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 11262 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 11262 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 11262 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 69017 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 69017 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 64326 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 64326 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 167775 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 167775 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 162255 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162255 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162283 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162283 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 178125 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178125 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 95380 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 95380 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 96218 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 96218 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 96537 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 96537 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 96712 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 96712 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 155248 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 155248 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 211766 None 0 Human Functional pEC50 = 7.4 7.4 -3 2
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 88905 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 88905 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 88920 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 88920 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 88924 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 88924 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 88936 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 88936 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 88994 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 88994 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 88998 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 88998 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 89303 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 89303 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 153055 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 153055 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 192561 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 192561 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 88885 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 88885 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 186900 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 186900 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 137877 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 137877 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 146281 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 146281 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 77259 None 1 Human Functional pEC50 = 8.4 8.4 - 1
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 77259 None 1 Human Functional pEC50 = 8.4 8.4 - 1
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 139564 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 139564 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 137877 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 137877 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 95770 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 95770 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 64843 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 64843 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 177421 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177421 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 96010 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 96010 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 167495 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 167495 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 99643 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 99643 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 99643 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 99643 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 10301 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 10301 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 177566 None 0 Human Functional pEC50 = 8.3 8.3 407 3
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177566 None 0 Human Functional pEC50 = 8.3 8.3 407 3
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 10301 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 10301 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 64611 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 64611 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 187178 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 187178 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 189102 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 189102 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 193064 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 193064 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 161100 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 161100 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 69036 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 69036 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 166575 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 166575 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 186894 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 186894 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 186989 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 186989 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 137107 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 137107 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 122999 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 122999 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 211766 None 0 Human Functional pEC50 = 7.4 7.4 -3 2
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 169042 None 0 Human Functional pEC50 = 5.4 5.4 -7 2
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 169042 None 0 Human Functional pEC50 = 5.4 5.4 -7 2
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 154671 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 154671 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 167451 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 167451 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 23868 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
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 23868 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
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 182377 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 182377 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 144993 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 144993 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 88573 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 88573 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 178125 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178125 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 122606 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 122606 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 12020 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 12020 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 12020 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 166662 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 166662 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 162255 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162255 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 186968 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 186968 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 115377 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 115377 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 11260 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 11260 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 11260 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 137810 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 137810 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 123553 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 123553 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 183571 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 183571 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 16465 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
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 16465 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
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 146570 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 146570 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 214220 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 214220 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 191655 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 191655 None 0 Human Functional pEC50 = 5.4 5.4 - 1
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 171438 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 171438 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 162053 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162053 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 172314 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 172314 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 166534 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 166534 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 166471 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 166471 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 90191 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 90191 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 137234 None 1 Human Functional pEC50 = 7.3 7.3 - 1
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 137234 None 1 Human Functional pEC50 = 7.3 7.3 - 1
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 69054 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 69054 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 209363 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 162660 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162660 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 10312 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 10312 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 138187 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 138187 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 139534 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 139534 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 169282 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 169282 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 71600 None 17 Human Functional pEC50 = 8.3 8.3 - 1
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 71600 None 17 Human Functional pEC50 = 8.3 8.3 - 1
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 71600 None 17 Human Functional pEC50 = 8.3 8.3 - 1
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 15528 None 0 Rat Functional pEC50 = 8.3 8.3 - 1
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 15528 None 0 Rat Functional pEC50 = 8.3 8.3 - 1
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 16849 None 0 Rat Functional pEC50 = 8.3 8.3 - 1
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 16849 None 0 Rat Functional pEC50 = 8.3 8.3 - 1
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 177121 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177121 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 94469 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 94469 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 162660 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162660 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 10312 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 10312 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 138187 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 138187 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 139534 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 139534 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 169282 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 169282 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 177121 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177121 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177566 None 0 Human Functional pEC50 = 8.3 8.3 407 3
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177566 None 0 Human Functional pEC50 = 8.3 8.3 407 3
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 190167 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 190167 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 88877 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 88877 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 88900 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 88900 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 88902 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 88902 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 88941 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 88941 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 88956 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 88956 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 88993 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 88993 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 89025 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 89025 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 79155 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 79155 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 79159 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 79159 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 147870 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 147870 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 209366 None 15 Human Functional pEC50 = 8.3 8.3 - 1
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 209366 None 15 Human Functional pEC50 = 8.3 8.3 - 1
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 10302 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 10302 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 62522 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 62522 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 10302 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 10302 None 0 Human Functional pEC50 = 8.3 8.3 - 1
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 209367 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 186923 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 186923 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 187017 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 187017 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 181115 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 181115 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 162053 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162053 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162838 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162838 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 88896 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 88896 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 88897 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 88897 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 88898 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 88898 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 88946 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 88946 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 88999 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 88999 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 89012 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 89012 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 89022 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 89022 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 193248 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 193248 None 0 Human Functional pEC50 = 5.3 5.3 - 1
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 147862 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 147862 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 69053 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 69053 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 167142 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 167142 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 148853 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 148853 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 162838 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162838 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 159943 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 159943 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 69058 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 69058 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 89908 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 89908 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 146532 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 146532 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 10311 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 10311 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 30445 None 0 Rat Functional pEC50 = 7.2 7.2 - 1
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 30445 None 0 Rat Functional pEC50 = 7.2 7.2 - 1
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 10311 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 10311 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 88489 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 88489 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 10310 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 10310 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 101239 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 101239 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 79151 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 79151 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 183302 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 183302 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 211757 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 113087 None 0 Rat Functional pEC50 = 8.2 8.2 - 1
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 113087 None 0 Rat Functional pEC50 = 8.2 8.2 - 1
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 10310 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 10310 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 10322 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 10322 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 101239 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 101239 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 145654 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 145654 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 178141 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178141 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 117011 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 117011 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 117011 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 117011 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 178141 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178141 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 161306 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 161306 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 192586 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 192586 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 211757 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 88887 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 88887 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 88926 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 88926 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 88930 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 88930 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 88986 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 88986 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 89003 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 89003 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 89006 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 89006 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 89030 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 89030 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 122144 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 122144 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 167454 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 167454 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 209364 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 95017 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 95017 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 187063 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 187063 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 167494 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 167494 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 2232 None 24 Rat Functional pEC50 = 7.2 7.2 1 5
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 2232 None 24 Rat Functional pEC50 = 7.2 7.2 1 5
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 2232 None 24 Rat Functional pEC50 = 7.2 7.2 1 5
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 166461 None 0 Rat Functional pEC50 = 7.2 7.2 - 1
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 166461 None 0 Rat Functional pEC50 = 7.2 7.2 - 1
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 121262 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 121262 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 184270 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 184270 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 155554 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 155554 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 183507 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 183507 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 209358 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 154766 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 154766 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 177906 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177906 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 97811 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 97811 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 121262 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 121262 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 211759 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 88876 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 88876 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 88886 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 88886 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 88987 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 88987 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 89001 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 89001 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 162789 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162789 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 137222 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 137222 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 97346 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
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 97346 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
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 162789 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162789 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 177575 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177575 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 95424 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 95424 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 5753 None 0 Human Functional pEC50 = 6.2 6.2 -125 2
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 5753 None 0 Human Functional pEC50 = 6.2 6.2 -125 2
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 167070 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 167070 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 95259 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 95259 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 136717 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 136717 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 136717 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 136717 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 29418 None 1 Rat Functional pEC50 = 7.2 7.2 - 1
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 29418 None 1 Rat Functional pEC50 = 7.2 7.2 - 1
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 3692 None 36 Human Functional pEC50 = 7.2 7.2 -128 11
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 3692 None 36 Human Functional pEC50 = 7.2 7.2 -128 11
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 3692 None 36 Human Functional pEC50 = 7.2 7.2 -128 11
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 3692 None 36 Human Functional pEC50 = 7.2 7.2 -128 11
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 3692 None 36 Human Functional pEC50 = 7.2 7.2 -128 11
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 175662 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 175662 None 0 Human Functional pEC50 = 5.2 5.2 - 1
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 89598 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 89598 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 166694 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 166694 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 69010 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 69010 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 11273 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 11273 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 11273 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 177575 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177575 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177906 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177906 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 12032 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 12032 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 12032 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 186821 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 186821 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 162182 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162182 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 177629 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177629 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 209364 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 209366 None 15 Human Functional pEC50 = 8.1 8.1 - 1
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 209366 None 15 Human Functional pEC50 = 8.1 8.1 - 1
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 63497 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 63497 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 64319 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 64319 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 141334 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 141334 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 141334 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 141334 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 96539 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 96539 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 63640 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 63640 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 63903 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 63903 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 178221 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178221 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 79162 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 79162 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 89900 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 89900 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 162182 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162182 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 177078 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177078 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177500 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177500 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177629 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177629 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178221 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 178221 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 183931 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 183931 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 184045 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 184045 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 88891 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 88891 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 88907 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 88907 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 88933 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 88933 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 88974 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 88974 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 88979 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 88979 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 88991 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 88991 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 89016 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 89016 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 12049 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 12049 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 12049 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 96299 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 96299 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 139692 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 139692 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 139692 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 139692 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 167204 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 167204 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 211759 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 215837 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 97011 None 0 Human Functional pEC50 = 6.1 6.1 1 2
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 97011 None 0 Human Functional pEC50 = 6.1 6.1 1 2
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 181986 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 181986 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 166450 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 166450 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 190577 None 0 Human Functional pEC50 = 4.1 4.1 - 1
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 190577 None 0 Human Functional pEC50 = 4.1 4.1 - 1
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 140061 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 140061 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 148176 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 148176 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 94619 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 94619 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 162283 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162283 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 174585 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 174585 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 69061 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 69061 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 202090 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 202090 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 202090 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 202090 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 186834 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 186834 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 148180 None 0 Human Functional pEC50 = 7.1 7.1 -3 2
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 148180 None 0 Human Functional pEC50 = 7.1 7.1 -3 2
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 148180 None 0 Human Functional pEC50 = 7.1 7.1 -3 2
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 148180 None 0 Human Functional pEC50 = 7.1 7.1 -3 2
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 162283 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 162283 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion 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 5854 None 0 Human Functional pEC50 = 7.1 7.1 -1 2
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 5854 None 0 Human Functional pEC50 = 7.1 7.1 -1 2
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 5976 None 0 Human Functional pEC50 = 7.1 7.1 -31 2
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 5976 None 0 Human Functional pEC50 = 7.1 7.1 -31 2
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 211765 None 0 Human Functional pEC50 = 7.1 7.1 -15 2
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 88890 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 88890 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 88944 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 88944 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 88975 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 88975 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 88992 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 88992 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 159776 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 159776 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 112879 None 0 Rat Functional pEC50 = 8.1 8.1 - 1
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 112879 None 0 Rat Functional pEC50 = 8.1 8.1 - 1
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 69052 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 69052 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 180052 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 180052 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 177500 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177500 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 160653 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 160653 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 10305 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 10305 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 10309 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 10309 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 10305 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 10305 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 10309 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 10309 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 180858 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 180858 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 146151 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 146151 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 177078 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 177078 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at 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 167952 None 0 Rat Functional pEC50 = 8.1 8.1 - 1
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 167952 None 0 Rat Functional pEC50 = 8.1 8.1 - 1
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 193249 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 193249 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 139734 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 139734 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 89739 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 89739 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 69011 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 69011 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 166832 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 166832 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 69064 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 69064 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 167138 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 167138 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 89302 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 89302 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 155121 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 155121 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 211765 None 0 Human Functional pEC50 = 7.1 7.1 -15 2
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 179836 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 179836 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 64283 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 64283 None 0 Human Functional pEC50 = 8.1 8.1 - 1
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 167952 None 0 Rat Functional pEC50 = 8.1 8.1 - 1
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 167952 None 0 Rat Functional pEC50 = 8.1 8.1 - 1
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 19451 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 19451 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 209354 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 89901 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 89901 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 63914 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 63914 None 0 Human Functional pEC50 = 8.0 8.0 - 1
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 79156 None 0 Human Functional pEC50 = 8 8.0 - 1
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 79156 None 0 Human Functional pEC50 = 8 8.0 - 1
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 184751 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 184751 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 186769 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 186769 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 192522 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 192522 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 186941 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 186941 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 186832 None 0 Human Functional pEC50 = 5.1 5.1 - 1
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 186832 None 0 Human Functional pEC50 = 5.1 5.1 - 1
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 166813 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 166813 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 166926 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 166926 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 209360 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 166890 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 166890 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 84844 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 84844 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 214133 None 23 Human Functional pEC50 = 7.0 7.0 - 1
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 145450 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 145450 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 145448 None 0 Human Functional pEC50 = 7 7.0 - 1
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 145448 None 0 Human Functional pEC50 = 7 7.0 - 1
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 211764 None 0 Human Functional pEC50 = 7 7.0 -33 2
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 212161 None 0 Rat Functional pED50 = 8 8.0 - 0
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 98225 None 0 Rat Functional pED50 = 6.7 6.7 - 1
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 98225 None 0 Rat Functional pED50 = 6.7 6.7 - 1
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 73198 None 0 Human Functional pIC50 = 9.7 9.7 - 1
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 73198 None 0 Human Functional pIC50 = 9.7 9.7 - 1
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 96932 None 0 Human Functional pIC50 = 9.5 9.5 - 1
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 96932 None 0 Human Functional pIC50 = 9.5 9.5 - 1
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 215578 None 0 Human Functional pIC50 = 9.5 9.5 - 1
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 113478 None 1 Human Functional pIC50 = 9.1 9.1 - 1
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 113478 None 1 Human Functional pIC50 = 9.1 9.1 - 1
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 81848 None 0 Human Functional pIC50 = 9 9.0 - 1
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 81848 None 0 Human Functional pIC50 = 9 9.0 - 1
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 73199 None 0 Human Functional pIC50 = 9 9.0 - 1
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 73199 None 0 Human Functional pIC50 = 9 9.0 - 1
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 113439 None 0 Human Functional pIC50 = 8.9 8.9 - 1
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 113439 None 0 Human Functional pIC50 = 8.9 8.9 - 1
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 77342 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 77342 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 65229 None 1 Human Functional pIC50 = 8 8.0 - 1
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 65229 None 1 Human Functional pIC50 = 8 8.0 - 1
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 77648 None 0 Human Functional pIC50 = 8 8.0 - 1
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 77648 None 0 Human Functional pIC50 = 8 8.0 - 1
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 75991 None 0 Human Functional pIC50 = 8 8.0 - 1
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 75991 None 0 Human Functional pIC50 = 8 8.0 - 1
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 123235 None 0 Human Functional pIC50 = 8 8.0 - 1
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 123235 None 0 Human Functional pIC50 = 8 8.0 - 1
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 141322 None 0 Human Functional pIC50 = 8 8.0 - 1
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 141322 None 0 Human Functional pIC50 = 8 8.0 - 1
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 139938 None 0 Human Functional pIC50 = 7 7.0 - 1
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 139938 None 0 Human Functional pIC50 = 7 7.0 - 1
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 5532 None 4 Human Functional pIC50 = 7 7.0 - 1
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 5532 None 4 Human Functional pIC50 = 7 7.0 - 1
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 122000 None 0 Rat Functional pIC50 = 7 7.0 -67 2
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 122000 None 0 Rat Functional pIC50 = 7 7.0 -67 2
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 121337 None 0 Human Functional pIC50 = 6 6.0 - 1
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 121337 None 0 Human Functional pIC50 = 6 6.0 - 1
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 66668 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 66668 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 124030 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 124030 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 122030 None 0 Human Functional pIC50 = 5.0 5.0 - 1
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 122030 None 0 Human Functional pIC50 = 5.0 5.0 - 1
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 167389 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 167389 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 80214 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 80214 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 121346 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 121346 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 77914 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 77914 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 139240 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 139240 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 76722 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 76722 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 73190 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 73190 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 76731 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 76731 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 75553 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 75553 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 75565 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 75565 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 81845 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 81845 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 81899 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 81899 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 81906 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 81906 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 121347 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 121347 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 214431 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 139660 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 139660 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 166957 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 166957 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 66160 None 1 Human Functional pIC50 = 6.9 6.9 - 1
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 66160 None 1 Human Functional pIC50 = 6.9 6.9 - 1
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 139970 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 139970 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 81835 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 81835 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 166769 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 166769 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 81837 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 81837 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 74999 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 74999 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 6265 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 6265 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 73201 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 73201 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 76765 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 76765 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 7595 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 7595 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 5909 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 5909 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 75012 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 75012 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 167138 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 167138 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 139931 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 139931 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 121348 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 121348 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 166534 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 166534 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 6375 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 6375 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 121350 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 121350 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 167211 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 167211 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 81849 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 81849 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 6143 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 6143 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 122007 None 0 Rat Functional pIC50 = 7.9 7.9 -8 2
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 122007 None 0 Rat Functional pIC50 = 7.9 7.9 -8 2
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 76340 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 76340 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 139717 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 139717 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 166744 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 166744 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 139970 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 139970 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 6103 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 6103 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 161312 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 161312 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 74685 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 74685 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 140844 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 140844 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 76256 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 76256 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 81903 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 81903 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 215578 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 62990 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 62990 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 75972 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 75972 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 75994 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 75994 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 6256 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 6256 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 81902 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 81902 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 140844 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 140844 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 76179 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 76179 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 5996 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 5996 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 73196 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 73196 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 67010 None 1 Human Functional pIC50 = 6.8 6.8 - 1
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 67010 None 1 Human Functional pIC50 = 6.8 6.8 - 1
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 211799 None 6 Rat Functional pIC50 = 6.8 6.8 - 1
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 6385 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 6385 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 81834 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 81834 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 166864 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 166864 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 126823 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 126823 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 215578 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 215578 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 215578 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 139975 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 139975 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 167314 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 167314 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 167316 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 167316 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 213927 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 75986 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 75986 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 64458 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 64458 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 73205 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 73205 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 215578 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 121346 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 121346 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 6141 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 6141 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 141007 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 141007 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 62574 None 1 Human Functional pIC50 = 5.8 5.8 - 1
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 62574 None 1 Human Functional pIC50 = 5.8 5.8 - 1
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 73193 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 73193 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 166694 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 166694 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 66338 None 1 Human Functional pIC50 = 7.8 7.8 - 1
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 66338 None 1 Human Functional pIC50 = 7.8 7.8 - 1
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 214133 None 23 Human Functional pIC50 = 7.8 7.8 - 1
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 62996 None 17 Human Functional pIC50 = 6.8 6.8 - 1
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 62996 None 17 Human Functional pIC50 = 6.8 6.8 - 1
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 165924 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 165924 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 165924 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 165924 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 62996 None 17 Human Functional pIC50 = 6.8 6.8 - 1
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 62996 None 17 Human Functional pIC50 = 6.8 6.8 - 1
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 75696 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 75696 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 166662 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 166662 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 141215 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 141215 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 78771 None 1 Human Functional pIC50 = 6.7 6.7 - 1
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 78771 None 1 Human Functional pIC50 = 6.7 6.7 - 1
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 62990 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 62990 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 125056 None 1 Human Functional pIC50 = 7.7 7.7 - 1
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 125056 None 1 Human Functional pIC50 = 7.7 7.7 - 1
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 74999 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 74999 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 76027 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 76027 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 125195 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 125195 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 76180 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 76180 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 214220 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 214220 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 66184 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 66184 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 75932 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 75932 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 139938 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 139938 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 137025 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 137025 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 167275 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 167275 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 121336 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 121336 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 73202 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 73202 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 125191 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 125191 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 125193 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 125193 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 139955 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 139955 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 125190 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 125190 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 139955 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 139955 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 73224 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 73224 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 6030 None 0 Rat Functional pIC50 = 8.7 8.7 4 2
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 6030 None 0 Rat Functional pIC50 = 8.7 8.7 4 2
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 121340 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 121340 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 6056 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 6056 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 121340 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 121340 None 0 Human Functional pIC50 = 8.7 8.7 - 1
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 73204 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 73204 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 73206 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 73206 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 214220 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 214220 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 121342 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 121342 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 6133 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 6133 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 6142 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 6142 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 73223 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 73223 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 167289 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 167289 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 121345 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 121345 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 75885 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 75885 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 214220 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 214220 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 214118 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 76742 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 76742 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 121348 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 121348 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 81836 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 81836 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 125195 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 125195 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 75525 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 75525 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 81838 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 81838 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 121335 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 121335 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 76638 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 76638 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 121349 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 121349 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 64871 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 64871 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 167002 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 167002 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 166953 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 166953 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 138397 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 138397 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 81843 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 81843 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 81908 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 81908 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 167204 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 167204 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 6374 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 6374 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 75864 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 75864 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 77882 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 77882 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 121345 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 121345 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 6233 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 6233 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 81844 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 81844 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 122032 None 12 Human Functional pIC50 = 6.6 6.6 - 1
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 122032 None 12 Human Functional pIC50 = 6.6 6.6 - 1
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 62503 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 62503 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 81910 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 81910 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 81900 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 81900 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 75394 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 75394 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 6187 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 6187 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 73195 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 73195 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 213960 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 214220 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 214220 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 167394 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 167394 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 81904 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 81904 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 137674 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 137674 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 81847 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 81847 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 215578 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 73194 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 73194 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 6367 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 6367 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 62597 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 62597 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 167258 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 167258 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 141251 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 141251 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 166579 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 166579 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 64458 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 64458 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 214220 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 214220 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 169552 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 169552 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 166813 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 166813 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 66136 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 66136 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 125190 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 125190 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 125192 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 125192 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 125194 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 125194 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 139860 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 139860 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 73192 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 73192 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 73226 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 73226 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 138533 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 138533 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 76005 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 76005 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 166926 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 166926 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 65202 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 65202 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 75884 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 75884 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 121585 None 0 Human Functional pIC50 = 7.5 7.5 8 2
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 121585 None 0 Human Functional pIC50 = 7.5 7.5 8 2
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 7610 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 7610 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 122166 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 122166 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 73208 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 73208 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 121349 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 121349 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 73200 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 73200 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 166575 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 166575 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 76533 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 76533 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 76257 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 76257 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 124379 None 2 Human Functional pIC50 = 6.5 6.5 - 1
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 124379 None 2 Human Functional pIC50 = 6.5 6.5 - 1
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 76670 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 76670 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 76023 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 76023 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 214220 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 214220 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 74419 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 74419 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 139975 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 139975 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 168711 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 168711 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 166450 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 166450 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 125196 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 125196 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 5908 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 5908 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 76199 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 76199 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 121334 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 121334 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 7594 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 7594 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 139253 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 139253 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 122006 None 0 Rat Functional pIC50 = 7.5 7.5 -7 2
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 122006 None 0 Rat Functional pIC50 = 7.5 7.5 -7 2
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 140716 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 140716 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 141504 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 141504 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 75506 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 75506 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 76740 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 76740 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 75967 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 75967 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 214220 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 214220 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 139941 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 139941 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 75548 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 75548 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 167343 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 167343 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 74999 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 74999 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 5907 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 5907 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 81841 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 81841 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 141363 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 141363 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 165824 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 165824 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 141249 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 141249 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 79899 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 79899 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 168336 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 168336 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 139612 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 139612 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 139705 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 139705 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 139860 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 139860 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 125191 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 125191 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 139705 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 139705 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 6096 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 6096 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 73207 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 73207 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 121332 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 121332 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 121342 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 121342 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 139296 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 139296 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 5626 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 5626 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 77141 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 77141 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 166914 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 166914 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 121350 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 121350 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 80215 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 80215 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 215578 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 64612 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 64612 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 139813 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 139813 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 139931 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 139931 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 121334 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 121334 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 76723 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 76723 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 7609 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 7609 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 6205 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 6205 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 121338 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 121338 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 139660 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 139660 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 214220 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 214220 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 76704 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 76704 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 123852 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 123852 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 166471 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 166471 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 5993 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 5993 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 81846 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 81846 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 81901 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 81901 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 62943 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 62943 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 77351 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 77351 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 77147 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 77147 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 64574 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 64574 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 67075 None 1 Human Functional pIC50 = 6.3 6.3 - 1
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 67075 None 1 Human Functional pIC50 = 6.3 6.3 - 1
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 211799 None 6 Rat Functional pIC50 = 8.3 8.3 - 1
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 121343 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 121343 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 76035 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 76035 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 141333 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 141333 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 73221 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 73221 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 83527 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 83527 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 121336 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 121336 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 62911 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 62911 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 168644 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 168644 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 81911 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 81911 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 138534 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 138534 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 166389 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 166389 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 126765 None 0 Human Functional pIC50 = 7.3 7.3 -5 3
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 126765 None 0 Human Functional pIC50 = 7.3 7.3 -5 3
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 74846 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 74846 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 166890 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 166890 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 124386 None 1 Human Functional pIC50 = 7.3 7.3 - 1
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 124386 None 1 Human Functional pIC50 = 7.3 7.3 - 1
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 79886 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 79886 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 66330 None 1 Human Functional pIC50 = 6.3 6.3 - 1
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 66330 None 1 Human Functional pIC50 = 6.3 6.3 - 1
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 66201 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 66201 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 166936 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 166936 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 75801 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 75801 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 76515 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 76515 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 166748 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 166748 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 6386 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 6386 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 73222 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 73222 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 121332 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 121332 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 215578 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 113447 None 18 Human Functional pIC50 = 8.2 8.2 - 1
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 113447 None 18 Human Functional pIC50 = 8.2 8.2 - 1
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 75983 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 75983 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 125196 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 125196 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 214220 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 214220 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 137034 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 137034 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 63076 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 63076 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 214220 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 214220 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 75063 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 75063 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 141798 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 141798 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 62502 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 62502 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 123856 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 123856 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 6140 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 6140 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 81842 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 81842 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 6266 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 6266 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 6019 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 6019 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 6369 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 6369 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 141366 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 141366 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 121338 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 121338 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 6368 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 6368 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 214148 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 166641 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 166641 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 64613 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 64613 None 0 Human Functional pIC50 = 5.2 5.2 - 1
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 75497 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 75497 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 75788 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 75788 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 75966 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 75966 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 220 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 220 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 220 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 79600 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 79600 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 121339 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 121339 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 139612 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 139612 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 6194 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 6194 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 81839 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 81839 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 73191 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 73191 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 73225 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 73225 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 73189 None 0 Mouse Functional pIC50 = 8.2 8.2 1 2
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 73189 None 0 Mouse Functional pIC50 = 8.2 8.2 1 2
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 166035 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 166035 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 166035 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 166035 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 121343 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 121343 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 121344 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 121344 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 139941 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 139941 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 139759 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 139759 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 77332 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 77332 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 81909 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 81909 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 127171 None 1 Human Functional pIC50 = 6.2 6.2 - 1
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 127171 None 1 Human Functional pIC50 = 6.2 6.2 - 1
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 76408 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 76408 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 81907 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 81907 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 121302 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 121302 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 77051 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 77051 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 64581 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 64581 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 123237 None 40 Human Functional pIC50 = 5.1 5.1 - 1
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 123237 None 40 Human Functional pIC50 = 5.1 5.1 - 1
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 6384 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 6384 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 121337 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 121337 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 140557 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 140557 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 75377 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 75377 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 170031 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 170031 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 73197 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 73197 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 121347 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 121347 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 75995 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 75995 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 167070 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 167070 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 124465 None 1 Human Functional pIC50 = 8.1 8.1 - 1
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 124465 None 1 Human Functional pIC50 = 8.1 8.1 - 1
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 125192 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 125192 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 125193 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 125193 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 124465 None 1 Human Functional pIC50 = 8.1 8.1 - 1
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 124465 None 1 Human Functional pIC50 = 8.1 8.1 - 1
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 73189 None 0 Human Functional pIC50 = 8.1 8.1 -1 2
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 73189 None 0 Human Functional pIC50 = 8.1 8.1 -1 2
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 73203 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 73203 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 121339 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 121339 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 167142 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 167142 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 141731 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 141731 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 166707 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 166707 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 215578 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 121302 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 121302 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 140898 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 140898 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 121333 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 121333 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 214220 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 214220 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 75507 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 75507 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 166832 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 166832 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 75370 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 75370 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 66911 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 66911 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 84679 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 84679 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 78549 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 78549 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 121335 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 121335 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 125194 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 125194 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 6257 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 6257 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 121344 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 121344 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 141317 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 141317 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 6030 None 0 Human Functional pIC50 = 8.0 8.0 -4 2
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 6030 None 0 Human Functional pIC50 = 8.0 8.0 -4 2
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 140883 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 140883 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 140485 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 140485 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 76748 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 76748 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 76176 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 76176 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 139717 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 139717 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 139759 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 139759 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 167019 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 167019 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 169221 None 1 Human Functional pIC50 = 7.0 7.0 - 1
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 169221 None 1 Human Functional pIC50 = 7.0 7.0 - 1
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 76425 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 76425 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 75985 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 75985 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 67113 None 1 Human Functional pIC50 = 7.0 7.0 - 1
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 67113 None 1 Human Functional pIC50 = 7.0 7.0 - 1
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 76016 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 76016 None 0 Human Functional pIC50 = 6.0 6.0 - 1
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 214093 None 0 Human Functional pIC50 = 6 6.0 - 1
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 172955 None 0 Human Functional pKd = 8.8 8.8 - 1
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 172955 None 0 Human Functional pKd = 8.8 8.8 - 1
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 172955 None 0 Human Functional pKd = 8.0 8.0 - 1
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 172955 None 0 Human Functional pKd = 8.0 8.0 - 1
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 174585 None 0 Human Functional pKd = 7.5 7.5 - 1
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 174585 None 0 Human Functional pKd = 7.5 7.5 - 1
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 174585 None 0 Human Functional pKd = 7.1 7.1 - 1
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 174585 None 0 Human Functional pKd = 7.1 7.1 - 1
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 69042 None 0 Human Functional pKi = 9 9.0 - 1
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 69042 None 0 Human Functional pKi = 9 9.0 - 1
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 83527 None 0 Human Functional pKi = 7 7.0 - 1
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 83527 None 0 Human Functional pKi = 7 7.0 - 1
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 155554 None 0 Human Functional pKi = 7.9 7.9 - 1
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 155554 None 0 Human Functional pKi = 7.9 7.9 - 1
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 155330 None 0 Human Functional pKi = 5.9 5.9 - 1
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 155330 None 0 Human Functional pKi = 5.9 5.9 - 1
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 95259 None 0 Human Functional pKi = 7.8 7.8 - 1
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 95259 None 0 Human Functional pKi = 7.8 7.8 - 1
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 97833 None 0 Human Functional pKi = 6.7 6.7 - 1
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 97833 None 0 Human Functional pKi = 6.7 6.7 - 1
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 89909 None 0 Human Functional pKi = 6.7 6.7 - 1
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 89909 None 0 Human Functional pKi = 6.7 6.7 - 1
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 159378 None 0 Human Functional pKi = 6.6 6.6 - 1
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 159378 None 0 Human Functional pKi = 6.6 6.6 - 1
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 97647 None 0 Human Functional pKi = 5.6 5.6 - 1
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 97647 None 0 Human Functional pKi = 5.6 5.6 - 1
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 155256 None 0 Human Functional pKi = 5.6 5.6 - 1
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 155256 None 0 Human Functional pKi = 5.6 5.6 - 1
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 88704 None 0 Human Functional pKi = 5.5 5.5 - 1
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 88704 None 0 Human Functional pKi = 5.5 5.5 - 1
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 155137 None 0 Human Functional pKi = 6.5 6.5 - 1
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 155137 None 0 Human Functional pKi = 6.5 6.5 - 1
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 155256 None 0 Human Functional pKi = 5.4 5.4 - 1
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 155256 None 0 Human Functional pKi = 5.4 5.4 - 1
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 97799 None 0 Human Functional pKi = 7.4 7.4 - 1
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 97799 None 0 Human Functional pKi = 7.4 7.4 - 1
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 97647 None 0 Human Functional pKi = 6.3 6.3 - 1
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 97647 None 0 Human Functional pKi = 6.3 6.3 - 1
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 97567 None 0 Human Functional pKi = 8.2 8.2 - 1
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 97567 None 0 Human Functional pKi = 8.2 8.2 - 1
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 97601 None 0 Human Functional pKi = 6.3 6.3 - 1
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 97601 None 0 Human Functional pKi = 6.3 6.3 - 1
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 69034 None 0 Human Functional pKi = 8.2 8.2 - 1
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 69034 None 0 Human Functional pKi = 8.2 8.2 - 1
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 97596 None 0 Human Functional pKi = 6.2 6.2 - 1
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 97596 None 0 Human Functional pKi = 6.2 6.2 - 1
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 155330 None 0 Human Functional pKi = 7.2 7.2 - 1
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 155330 None 0 Human Functional pKi = 7.2 7.2 - 1
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 95259 None 0 Human Functional pKi = 6.2 6.2 - 1
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 95259 None 0 Human Functional pKi = 6.2 6.2 - 1
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 155601 None 0 Human Functional pKi = 8.1 8.1 - 1
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 155601 None 0 Human Functional pKi = 8.1 8.1 - 1
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 155554 None 0 Human Functional pKi = 6.1 6.1 - 1
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 155554 None 0 Human Functional pKi = 6.1 6.1 - 1
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 1784 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 2232 None 24 Human Functional pEC50 = 7 7.0 -3 5
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 2232 None 24 Human Functional pEC50 = 7 7.0 -3 5
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 2232 None 24 Human Functional pEC50 = 7 7.0 -3 5
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 4078 None 0 Human Functional pEC50 = 7.2 7.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21402696
121879 2232 None 24 Rat Functional pEC50 = 7.2 7.2 1 5
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 2232 None 24 Rat Functional pEC50 = 7.2 7.2 1 5
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 2232 None 24 Rat Functional pEC50 = 7.2 7.2 1 5
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 1784 None 0 Human Functional pEC50 = 7.4 7.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10628755
1099 1784 None 0 Human Functional pEC50 = 7.4 7.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
121879 2232 None 24 Human Functional pEC50 = 7.5 7.5 -3 5
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 2232 None 24 Human Functional pEC50 = 7.5 7.5 -3 5
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 2232 None 24 Human Functional pEC50 = 7.5 7.5 -3 5
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 1792 None 0 Human Functional pEC50 = 8.3 8.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
4345065 1792 None 0 Human Functional pEC50 = 8.3 8.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
1093 1792 None 0 Human Functional pEC50 = 9.1 9.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
4345065 1792 None 0 Human Functional pEC50 = 9.1 9.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
178024 1969 None 33 Human Functional pEC50 = 9.2 9.2 -1 3
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 1969 None 33 Human Functional pEC50 = 9.2 9.2 -1 3
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 1969 None 33 Human Functional pEC50 = 9.2 9.2 -1 3
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 1969 None 33 Human Functional pEC50 = 9.2 9.2 -1 3
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 1969 None 33 Human Functional pEC50 = 9.2 9.2 -1 3
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 1969 None 33 Human Functional pEC50 = 9.2 9.2 -1 3
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 1784 None 0 Human Functional pEC50 = 9.5 9.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12907757
1099 1784 None 0 Human Functional pEC50 = 9.5 9.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21402696
5866 3622 None 4 Human Functional pEC50 = 9.5 9.5 - 1
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 3622 None 4 Human Functional pEC50 = 9.5 9.5 - 1
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 3622 None 4 Human Functional pEC50 = 9.5 9.5 - 1
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 2328 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 220 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 220 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 220 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 2122 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 2122 None 0 Human Functional pIC50 = 8.3 8.3 - 1
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 1872 None 8 Human Functional pIC50 = 8.4 8.4 2 2
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 1872 None 8 Human Functional pIC50 = 8.4 8.4 2 2
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 1872 None 8 Human Functional pIC50 = 8.4 8.4 2 2
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 3622 None 4 Human Functional pIC50 = 8.9 8.9 - 1
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 3622 None 4 Human Functional pIC50 = 8.9 8.9 - 1
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 3622 None 4 Human Functional pIC50 = 8.9 8.9 - 1
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 1872 None 8 Rat Functional pKB = 8 8.0 -2 2
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 1872 None 8 Rat Functional pKB = 8 8.0 -2 2
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 1872 None 8 Rat Functional pKB = 8 8.0 -2 2
UnclassifiedUnclassified
Guide to Pharmacology 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 21034740


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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type		 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
2713 205269 None 82 Human Binding pAC50 = 6 6.0 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5353524 205269 None 82 Human Binding pAC50 = 6 6.0 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5360566 205269 None 82 Human Binding pAC50 = 6 6.0 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
88536661 205269 None 82 Human Binding pAC50 = 6 6.0 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
9552079 205269 None 82 Human Binding pAC50 = 6 6.0 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1330113 205269 None 82 Human Binding pAC50 = 6 6.0 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL790 205269 None 82 Human Binding pAC50 = 6 6.0 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
156419 937 None 74 Human Binding pAC50 = 5 5.0 - 1
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
3308 937 None 74 Human Binding pAC50 = 5 5.0 - 1
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
647 937 None 74 Human Binding pAC50 = 5 5.0 - 1
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL1201284 937 None 74 Human Binding pAC50 = 5 5.0 - 1
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
DB01012 937 None 74 Human Binding pAC50 = 5 5.0 - 1
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
5920 47273 None 83 Human Binding pAC50 = 5.0 5.0 - 1
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 651 5 3 4 4.0 N[C@@H](Cc1cc(I)c(Oc2ccc(O)c(I)c2)c(I)c1)C(=O)O 10.1038/s41467-023-40064-9
7048703 47273 None 83 Human Binding pAC50 = 5.0 5.0 - 1
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 651 5 3 4 4.0 N[C@@H](Cc1cc(I)c(Oc2ccc(O)c(I)c2)c(I)c1)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL1544 47273 None 83 Human Binding pAC50 = 5.0 5.0 - 1
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 651 5 3 4 4.0 N[C@@H](Cc1cc(I)c(Oc2ccc(O)c(I)c2)c(I)c1)C(=O)O 10.1038/s41467-023-40064-9
148192 10418 None 81 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 704 14 5 9 4.2 COC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)[C@@H](O)CN(Cc1ccc(-c2ccccn2)cc1)NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)C(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL1163 10418 None 81 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 704 14 5 9 4.2 COC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)[C@@H](O)CN(Cc1ccc(-c2ccccn2)cc1)NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)C(C)(C)C 10.1038/s41467-023-40064-9
154257 178617 None 67 Human Binding pAC50 = 6.0 6.0 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
CHEMBL46740 178617 None 67 Human Binding pAC50 = 6.0 6.0 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
2600 3777 None 74 Human Binding pAC50 = 5.0 5.0 - 13
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 3777 None 74 Human Binding pAC50 = 5.0 5.0 - 13
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 3777 None 74 Human Binding pAC50 = 5.0 5.0 - 13
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 3777 None 74 Human Binding pAC50 = 5.0 5.0 - 13
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 3777 None 74 Human Binding pAC50 = 5.0 5.0 - 13
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
47319 26462 None 35 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 929 24 0 12 8.1 COc1ccc(CC2c3cc(OC)c(OC)cc3CC[N+]2(C)CCC(=O)OCCCCCOC(=O)CC[N+]2(C)CCc3cc(OC)c(OC)cc3C2Cc2ccc(OC)c(OC)c2)cc1OC 10.1038/s41467-023-40064-9
CHEMBL1360 26462 None 35 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 929 24 0 12 8.1 COc1ccc(CC2c3cc(OC)c(OC)cc3CC[N+]2(C)CCC(=O)OCCCCCOC(=O)CC[N+]2(C)CCc3cc(OC)c(OC)cc3C2Cc2ccc(OC)c(OC)c2)cc1OC 10.1038/s41467-023-40064-9
135409453 3771 None 41 Human Binding pAC50 = 5.0 5.0 - 2
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 3771 None 41 Human Binding pAC50 = 5.0 5.0 - 2
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 3771 None 41 Human Binding pAC50 = 5.0 5.0 - 2
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
71496458 115562 None 87 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
CHEMBL3353410 115562 None 87 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
242 470 None 124 Human Binding pAC50 = 4.9 4.9 - 52
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 470 None 124 Human Binding pAC50 = 4.9 4.9 - 52
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 470 None 124 Human Binding pAC50 = 4.9 4.9 - 52
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 470 None 124 Human Binding pAC50 = 4.9 4.9 - 52
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 470 None 124 Human Binding pAC50 = 4.9 4.9 - 52
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
39186 85933 None 54 Human Binding pAC50 = 4.9 4.9 - 2
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 414 6 0 6 3.4 COc1ccc([C@@H]2Sc3ccccc3N(CCN(C)C)C(=O)[C@@H]2OC(C)=O)cc1 10.1038/s41467-023-40064-9
CHEMBL23 85933 None 54 Human Binding pAC50 = 4.9 4.9 - 2
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 414 6 0 6 3.4 COc1ccc([C@@H]2Sc3ccccc3N(CCN(C)C)C(=O)[C@@H]2OC(C)=O)cc1 10.1038/s41467-023-40064-9
16362 3123 None 71 Human Binding pAC50 = 4.9 4.9 - 30
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2172 3123 None 71 Human Binding pAC50 = 4.9 4.9 - 30
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
90 3123 None 71 Human Binding pAC50 = 4.9 4.9 - 30
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1423 3123 None 71 Human Binding pAC50 = 4.9 4.9 - 30
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01100 3123 None 71 Human Binding pAC50 = 4.9 4.9 - 30
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
3042 1413 None 35 Human Binding pAC50 = 4.9 4.9 - 15
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
355 1413 None 35 Human Binding pAC50 = 4.9 4.9 - 15
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
868 1413 None 35 Human Binding pAC50 = 4.9 4.9 - 15
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
CHEMBL1123 1413 None 35 Human Binding pAC50 = 4.9 4.9 - 15
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
DB00804 1413 None 35 Human Binding pAC50 = 4.9 4.9 - 15
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
10184665 3989 None 51 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
4799 3989 None 51 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
7353 3989 None 51 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
CHEMBL1198857 3989 None 51 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
DB09082 3989 None 51 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
3191 102856 None 97 Human Binding pAC50 = 4.9 4.9 - 25
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
CHEMBL305660 102856 None 97 Human Binding pAC50 = 4.9 4.9 - 25
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
DB11742 102856 None 97 Human Binding pAC50 = 4.9 4.9 - 25
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
3926 207239 None 40 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 491 9 1 3 5.8 Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL92870 207239 None 40 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 491 9 1 3 5.8 Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
11626560 200935 None 94 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
CHEMBL601719 200935 None 94 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
2267 559 None 71 Human Binding pAC50 = 4.9 4.9 - 7
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
271 559 None 71 Human Binding pAC50 = 4.9 4.9 - 7
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
7121 559 None 71 Human Binding pAC50 = 4.9 4.9 - 7
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL639 559 None 71 Human Binding pAC50 = 4.9 4.9 - 7
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
DB00972 559 None 71 Human Binding pAC50 = 4.9 4.9 - 7
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
135564886 14491 None 5 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
135673376 14491 None 5 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
137157436 14491 None 5 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
145948239 14491 None 5 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
71587099 14491 None 5 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
CHEMBL1201304 14491 None 5 Human Binding pAC50 = 4.9 4.9 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
2585 802 None 103 Human Binding pAC50 = 4.9 4.9 - 22
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
522 802 None 103 Human Binding pAC50 = 4.9 4.9 - 22
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
551 802 None 103 Human Binding pAC50 = 4.9 4.9 - 22
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
CHEMBL723 802 None 103 Human Binding pAC50 = 4.9 4.9 - 22
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
DB01136 802 None 103 Human Binding pAC50 = 4.9 4.9 - 22
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
1353 1909 None 93 Human Binding pAC50 = 4.9 4.9 - 86
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 1909 None 93 Human Binding pAC50 = 4.9 4.9 - 86
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 1909 None 93 Human Binding pAC50 = 4.9 4.9 - 86
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 1909 None 93 Human Binding pAC50 = 4.9 4.9 - 86
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 1909 None 93 Human Binding pAC50 = 4.9 4.9 - 86
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
100 3803 None 58 Human Binding pAC50 = 4.8 4.8 - 55
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
2637 3803 None 58 Human Binding pAC50 = 4.8 4.8 - 55
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
5452 3803 None 58 Human Binding pAC50 = 4.8 4.8 - 55
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
CHEMBL479 3803 None 58 Human Binding pAC50 = 4.8 4.8 - 55
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
DB00679 3803 None 58 Human Binding pAC50 = 4.8 4.8 - 55
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
202 1507 None 77 Human Binding pAC50 = 4.8 4.8 - 33
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
60835 1507 None 77 Human Binding pAC50 = 4.8 4.8 - 33
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
972 1507 None 77 Human Binding pAC50 = 4.8 4.8 - 33
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1175 1507 None 77 Human Binding pAC50 = 4.8 4.8 - 33
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
DB00476 1507 None 77 Human Binding pAC50 = 4.8 4.8 - 33
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
11976 919 None 59 Human Binding pAC50 = 4.8 4.8 - 24
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
667467 919 None 59 Human Binding pAC50 = 4.8 4.8 - 24
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
CHEMBL908 919 None 59 Human Binding pAC50 = 4.8 4.8 - 24
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
DB01239 919 None 59 Human Binding pAC50 = 4.8 4.8 - 24
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
2218 15281 None 23 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 322 8 0 2 4.4 CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1 10.1038/s41467-023-40064-9
CHEMBL1213033 15281 None 23 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 322 8 0 2 4.4 CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1 10.1038/s41467-023-40064-9
41684 31219 None 105 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
CHEMBL1401 31219 None 105 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
3025 7273 None 86 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 10 1 4 3.5 CCCCOc1cc(C(=O)NCCN(CC)CC)c2ccccc2n1 10.1038/s41467-023-40064-9
CHEMBL1086 7273 None 86 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 10 1 4 3.5 CCCCOc1cc(C(=O)NCCN(CC)CC)c2ccccc2n1 10.1038/s41467-023-40064-9
44112 121288 None 48 Human Binding pAC50 = 4.8 4.8 - 7
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 10.1038/s41467-023-40064-9
CHEMBL357995 121288 None 48 Human Binding pAC50 = 4.8 4.8 - 7
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 10.1038/s41467-023-40064-9
68617 205525 None 62 Human Binding pAC50 = 4.8 4.8 - 26
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1709 205525 None 62 Human Binding pAC50 = 4.8 4.8 - 26
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL809 205525 None 62 Human Binding pAC50 = 4.8 4.8 - 26
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
2726 918 None 68 Human Binding pAC50 = 4.8 4.8 - 73
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 918 None 68 Human Binding pAC50 = 4.8 4.8 - 73
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 918 None 68 Human Binding pAC50 = 4.8 4.8 - 73
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 918 None 68 Human Binding pAC50 = 4.8 4.8 - 73
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 918 None 68 Human Binding pAC50 = 4.8 4.8 - 73
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
16363 595 None 53 Human Binding pAC50 = 4.8 4.8 - 7
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
312 595 None 53 Human Binding pAC50 = 4.8 4.8 - 7
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
9215 595 None 53 Human Binding pAC50 = 4.8 4.8 - 7
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL297302 595 None 53 Human Binding pAC50 = 4.8 4.8 - 7
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB12867 595 None 53 Human Binding pAC50 = 4.8 4.8 - 7
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2291 3182 None 58 Human Binding pAC50 = 4.8 4.8 - 12
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
2561 3182 None 58 Human Binding pAC50 = 4.8 4.8 - 12
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
4932 3182 None 58 Human Binding pAC50 = 4.8 4.8 - 12
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL631 3182 None 58 Human Binding pAC50 = 4.8 4.8 - 12
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
DB01182 3182 None 58 Human Binding pAC50 = 4.8 4.8 - 12
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
24826799 10796 None 104 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 532 4 1 6 4.5 Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12 10.1038/s41467-023-40064-9
CHEMBL1171837 10796 None 104 Human Binding pAC50 = 4.8 4.8 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 532 4 1 6 4.5 Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12 10.1038/s41467-023-40064-9
2274 3171 None 58 Human Binding pAC50 = 4.7 4.7 - 32
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4917 3171 None 58 Human Binding pAC50 = 4.7 4.7 - 32
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
7279 3171 None 58 Human Binding pAC50 = 4.7 4.7 - 32
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL728 3171 None 58 Human Binding pAC50 = 4.7 4.7 - 32
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00433 3171 None 58 Human Binding pAC50 = 4.7 4.7 - 32
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
2398 953 None 62 Human Binding pAC50 = 4.7 4.7 - 29
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801 953 None 62 Human Binding pAC50 = 4.7 4.7 - 29
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
701 953 None 62 Human Binding pAC50 = 4.7 4.7 - 29
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL415 953 None 62 Human Binding pAC50 = 4.7 4.7 - 29
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB01242 953 None 62 Human Binding pAC50 = 4.7 4.7 - 29
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
4046 2481 None 33 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4252 2481 None 33 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
CHEMBL416956 2481 None 33 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
DB00358 2481 None 33 Human Binding pAC50 = 4.7 4.7 - 2
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
3074 17956 None 26 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 604 16 0 12 3.5 COc1cc(C(=O)OCCCN2CCCN(CCCOC(=O)c3cc(OC)c(OC)c(OC)c3)CC2)cc(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL126075 17956 None 26 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 604 16 0 12 3.5 COc1cc(C(=O)OCCCN2CCCN(CCCOC(=O)c3cc(OC)c(OC)c(OC)c3)CC2)cc(OC)c1OC 10.1038/s41467-023-40064-9
4413 98071 None 57 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 347 4 5 4 2.6 N=C(N)Nc1ccc(C(=O)Oc2ccc3cc(C(=N)N)ccc3c2)cc1 10.1038/s41467-023-40064-9
CHEMBL273264 98071 None 57 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 347 4 5 4 2.6 N=C(N)Nc1ccc(C(=O)Oc2ccc3cc(C(=N)N)ccc3c2)cc1 10.1038/s41467-023-40064-9
25382 9155 None 37 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL110094 9155 None 37 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
2375 158392 None 106 Human Binding pAC50 = 5.7 5.7 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 430 5 2 5 2.9 CC(O)(CS(=O)(=O)c1ccc(F)cc1)C(=O)Nc1ccc(C#N)c(C(F)(F)F)c1 10.1038/s41467-023-40064-9
CHEMBL409 158392 None 106 Human Binding pAC50 = 5.7 5.7 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 430 5 2 5 2.9 CC(O)(CS(=O)(=O)c1ccc(F)cc1)C(=O)Nc1ccc(C#N)c(C(F)(F)F)c1 10.1038/s41467-023-40064-9
2351 4298 None 49 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1008 4298 None 49 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1257078 4298 None 49 Human Binding pAC50 = 4.7 4.7 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
448537 160248 None 89 Human Binding pAC50 = 4.7 4.7 - 25
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL411 160248 None 89 Human Binding pAC50 = 4.7 4.7 - 25
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 10.1038/s41467-023-40064-9
3393 207922 None 24 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 387 6 0 3 4.0 CCN(CC)CCN1C(=O)CN=C(c2ccccc2F)c2cc(Cl)ccc21 10.1038/s41467-023-40064-9
CHEMBL968 207922 None 24 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 387 6 0 3 4.0 CCN(CC)CCN1C(=O)CN=C(c2ccccc2F)c2cc(Cl)ccc21 10.1038/s41467-023-40064-9
441243 9834 None 58 Human Binding pAC50 = 4.6 4.6 - 8
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 670 12 5 7 3.1 CC(C)(C)NC(=O)[C@@H]1C[C@@H]2CCCC[C@@H]2CN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)c1ccc2ccccc2n1 10.1038/s41467-023-40064-9
CHEMBL114 9834 None 58 Human Binding pAC50 = 4.6 4.6 - 8
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 670 12 5 7 3.1 CC(C)(C)NC(=O)[C@@H]1C[C@@H]2CCCC[C@@H]2CN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)c1ccc2ccccc2n1 10.1038/s41467-023-40064-9
214 3858 None 58 Human Binding pAC50 = 4.6 4.6 - 30
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 3858 None 58 Human Binding pAC50 = 4.6 4.6 - 30
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 3858 None 58 Human Binding pAC50 = 4.6 4.6 - 30
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 3858 None 58 Human Binding pAC50 = 4.6 4.6 - 30
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 3858 None 58 Human Binding pAC50 = 4.6 4.6 - 30
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 3858 None 58 Human Binding pAC50 = 4.6 4.6 - 30
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
3036780 107529 None 20 Human Binding pAC50 = 4.6 4.6 - 54
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
46780481 107529 None 20 Human Binding pAC50 = 4.6 4.6 - 54
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
9903970 107529 None 20 Human Binding pAC50 = 4.6 4.6 - 54
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3187365 107529 None 20 Human Binding pAC50 = 4.6 4.6 - 54
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3544974 107529 None 20 Human Binding pAC50 = 4.6 4.6 - 54
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL504548 107529 None 20 Human Binding pAC50 = 4.6 4.6 - 54
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
DB06216 107529 None 20 Human Binding pAC50 = 4.6 4.6 - 54
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
6436173 55114 None 45 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL1617 55114 None 45 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
8550 14422 None 57 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 578 7 1 9 4.2 COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5ccccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC 10.1038/s41467-023-40064-9
CHEMBL1200515 14422 None 57 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 578 7 1 9 4.2 COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5ccccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC 10.1038/s41467-023-40064-9
31101 728 None 40 Human Binding pAC50 = 4.6 4.6 - 36
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
35 728 None 40 Human Binding pAC50 = 4.6 4.6 - 36
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
403 728 None 40 Human Binding pAC50 = 4.6 4.6 - 36
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
CHEMBL493 728 None 40 Human Binding pAC50 = 4.6 4.6 - 36
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
DB01200 728 None 40 Human Binding pAC50 = 4.6 4.6 - 36
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
104850 3328 None 96 Human Binding pAC50 = 4.6 4.6 - 6
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
4150 3328 None 96 Human Binding pAC50 = 4.6 4.6 - 6
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
743 3328 None 96 Human Binding pAC50 = 4.6 4.6 - 6
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL111 3328 None 96 Human Binding pAC50 = 4.6 4.6 - 6
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
DB06155 3328 None 96 Human Binding pAC50 = 4.6 4.6 - 6
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
392622 56310 None 95 Human Binding pAC50 = 4.6 4.6 - 4
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
CHEMBL163 56310 None 95 Human Binding pAC50 = 4.6 4.6 - 4
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
2995 204403 None 53 Human Binding pAC50 = 4.6 4.6 - 23
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1696 204403 None 53 Human Binding pAC50 = 4.6 4.6 - 23
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL72 204403 None 53 Human Binding pAC50 = 4.6 4.6 - 23
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
DB01151 204403 None 53 Human Binding pAC50 = 4.6 4.6 - 23
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
3947 206393 None 53 Human Binding pAC50 = 4.6 4.6 - 16
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL87708 206393 None 53 Human Binding pAC50 = 4.6 4.6 - 16
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
212 3804 None 47 Human Binding pAC50 = 4.6 4.6 - 25
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2639 3804 None 47 Human Binding pAC50 = 4.6 4.6 - 25
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651 3804 None 47 Human Binding pAC50 = 4.6 4.6 - 25
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL1201 3804 None 47 Human Binding pAC50 = 4.6 4.6 - 25
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01623 3804 None 47 Human Binding pAC50 = 4.6 4.6 - 25
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
73348210 210947 None 0 Human Binding pAC50 = 6.6 6.6 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](c2ccccc2)NC(=O)[C@@H]2C[C@H](OC(=O)NCCN)CN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(OCc3ccccc3)cc2)NC1=O 10.1038/s41467-023-40064-9
CHEMBL3039583 210947 None 0 Human Binding pAC50 = 6.6 6.6 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](c2ccccc2)NC(=O)[C@@H]2C[C@H](OC(=O)NCCN)CN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(OCc3ccccc3)cc2)NC1=O 10.1038/s41467-023-40064-9
60065 84367 None 6 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 505 7 1 8 4.2 COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@@H]2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL2218858 84367 None 6 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 505 7 1 8 4.2 COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@@H]2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
3081361 93932 None 123 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
CHEMBL24828 93932 None 123 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
107771 120246 None 49 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 517 7 2 7 6.1 COc1ccc2nc3cc(Cl)ccc3c(Nc3cc(CN4CCCC4)c(O)c(CN4CCCC4)c3)c2n1 10.1038/s41467-023-40064-9
CHEMBL35228 120246 None 49 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 517 7 2 7 6.1 COc1ccc2nc3cc(Cl)ccc3c(Nc3cc(CN4CCCC4)c(O)c(CN4CCCC4)c3)c2n1 10.1038/s41467-023-40064-9
3151 1461 None 97 Human Binding pAC50 = 4.6 4.6 - 27
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
945 1461 None 97 Human Binding pAC50 = 4.6 4.6 - 27
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
965 1461 None 97 Human Binding pAC50 = 4.6 4.6 - 27
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL219916 1461 None 97 Human Binding pAC50 = 4.6 4.6 - 27
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01184 1461 None 97 Human Binding pAC50 = 4.6 4.6 - 27
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
3949 100612 None 50 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 468 8 0 5 4.9 COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL29188 100612 None 50 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 468 8 0 5 4.9 COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC 10.1038/s41467-023-40064-9
2435 3588 None 83 Human Binding pAC50 = 4.6 4.6 - 49
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
60149 3588 None 83 Human Binding pAC50 = 4.6 4.6 - 49
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
98 3588 None 83 Human Binding pAC50 = 4.6 4.6 - 49
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
CHEMBL12713 3588 None 83 Human Binding pAC50 = 4.6 4.6 - 49
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
DB06144 3588 None 83 Human Binding pAC50 = 4.6 4.6 - 49
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
25181577 78217 None 56 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 574 9 2 9 5.0 CCOC(=O)[C@@H](N)Cc1ccc(-c2cc(O[C@H](c3ccc(Cl)cc3-n3ccc(C)n3)C(F)(F)F)nc(N)n2)cc1 10.1038/s41467-023-40064-9
CHEMBL2105695 78217 None 56 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 574 9 2 9 5.0 CCOC(=O)[C@@H](N)Cc1ccc(-c2cc(O[C@H](c3ccc(Cl)cc3-n3ccc(C)n3)C(F)(F)F)nc(N)n2)cc1 10.1038/s41467-023-40064-9
2318 154854 None 29 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 351 7 1 3 4.1 CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL400599 154854 None 29 Human Binding pAC50 = 4.6 4.6 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 351 7 1 3 4.1 CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1 10.1038/s41467-023-40064-9
2407 3370 None 76 Human Binding pAC50 = 4.5 4.5 - 7
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
59227 3370 None 76 Human Binding pAC50 = 4.5 4.5 - 7
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
941 3370 None 76 Human Binding pAC50 = 4.5 4.5 - 7
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
CHEMBL1303 3370 None 76 Human Binding pAC50 = 4.5 4.5 - 7
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
DB05271 3370 None 76 Human Binding pAC50 = 4.5 4.5 - 7
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
3380 22788 None 34 Human Binding pAC50 = 4.5 4.5 - 1
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 2 0 4 2.5 CN1C(=O)CN=C(c2ccccc2F)c2cc([N+](=O)[O-])ccc21 10.1038/s41467-023-40064-9
CHEMBL13280 22788 None 34 Human Binding pAC50 = 4.5 4.5 - 1
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 2 0 4 2.5 CN1C(=O)CN=C(c2ccccc2F)c2cc([N+](=O)[O-])ccc21 10.1038/s41467-023-40064-9
2202 3130 None 96 Human Binding pAC50 = 4.5 4.5 - 21
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
4850 3130 None 96 Human Binding pAC50 = 4.5 4.5 - 21
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
49 3130 None 96 Human Binding pAC50 = 4.5 4.5 - 21
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
CHEMBL1371770 3130 None 96 Human Binding pAC50 = 4.5 4.5 - 21
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
DB12478 3130 None 96 Human Binding pAC50 = 4.5 4.5 - 21
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
4495 196533 None 92 Human Binding pAC50 = 4.5 4.5 - 30
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL56367 196533 None 92 Human Binding pAC50 = 4.5 4.5 - 30
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 10.1038/s41467-023-40064-9
9801 91583 None 35 Human Binding pAC50 = 5.5 5.5 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 329 8 1 1 5.4 CC(Cc1ccccc1)NCCC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL24072 91583 None 35 Human Binding pAC50 = 5.5 5.5 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 329 8 1 1 5.4 CC(Cc1ccccc1)NCCC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
6729 14483 None 41 Human Binding pAC50 = 4.5 4.5 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 432 5 0 2 6.5 CC(C)(C)c1ccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)cc1 10.1038/s41467-023-40064-9
CHEMBL1201271 14483 None 41 Human Binding pAC50 = 4.5 4.5 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 432 5 0 2 6.5 CC(C)(C)c1ccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)cc1 10.1038/s41467-023-40064-9
DB00354 14483 None 41 Human Binding pAC50 = 4.5 4.5 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 432 5 0 2 6.5 CC(C)(C)c1ccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)cc1 10.1038/s41467-023-40064-9
1016 3745 None 78 Human Binding pAC50 = 4.5 4.5 - 35
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
2561 3745 None 78 Human Binding pAC50 = 4.5 4.5 - 35
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
2733526 3745 None 78 Human Binding pAC50 = 4.5 4.5 - 35
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
5384 3745 None 78 Human Binding pAC50 = 4.5 4.5 - 35
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL83 3745 None 78 Human Binding pAC50 = 4.5 4.5 - 35
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
DB00675 3745 None 78 Human Binding pAC50 = 4.5 4.5 - 35
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
9915743 63540 None 93 Human Binding pAC50 = 5.5 5.5 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 556 11 2 8 5.9 CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)/C=C/CN(C)C 10.1038/s41467-023-40064-9
CHEMBL180022 63540 None 93 Human Binding pAC50 = 5.5 5.5 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 556 11 2 8 5.9 CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)/C=C/CN(C)C 10.1038/s41467-023-40064-9
275196 125671 None 52 Human Binding pAC50 = 6.5 6.5 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 4 0 8 2.9 COc1ccc2c(c1OC)C(=O)O[C@@H]2[C@H]1c2c(cc3c(c2OC)OCO3)CCN1C 10.1038/s41467-023-40064-9
CHEMBL364713 125671 None 52 Human Binding pAC50 = 6.5 6.5 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 4 0 8 2.9 COc1ccc2c(c1OC)C(=O)O[C@@H]2[C@H]1c2c(cc3c(c2OC)OCO3)CCN1C 10.1038/s41467-023-40064-9
26987 948 None 33 Human Binding pAC50 = 5.5 5.5 - 21
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
6063 948 None 33 Human Binding pAC50 = 5.5 5.5 - 21
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
671 948 None 33 Human Binding pAC50 = 5.5 5.5 - 21
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
CHEMBL1626 948 None 33 Human Binding pAC50 = 5.5 5.5 - 21
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
DB00283 948 None 33 Human Binding pAC50 = 5.5 5.5 - 21
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
11980903 14490 None 19 Human Binding pAC50 = 5.4 5.4 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
22526 14490 None 19 Human Binding pAC50 = 5.4 5.4 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
5281035 14490 None 19 Human Binding pAC50 = 5.4 5.4 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201303 14490 None 19 Human Binding pAC50 = 5.4 5.4 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
25077405 2713 None 0 Human Binding pAC50 = 5.4 5.4 - 1
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
3902 2713 None 0 Human Binding pAC50 = 5.4 5.4 - 1
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
49800011 2713 None 0 Human Binding pAC50 = 5.4 5.4 - 1
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
CHEMBL1201309 2713 None 0 Human Binding pAC50 = 5.4 5.4 - 1
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
DB00666 2713 None 0 Human Binding pAC50 = 5.4 5.4 - 1
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
102 4125 None 48 Human Binding pAC50 = 5.4 5.4 - 50
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
3659 4125 None 48 Human Binding pAC50 = 5.4 5.4 - 50
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
8969 4125 None 48 Human Binding pAC50 = 5.4 5.4 - 50
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL15245 4125 None 48 Human Binding pAC50 = 5.4 5.4 - 50
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
DB01392 4125 None 48 Human Binding pAC50 = 5.4 5.4 - 50
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
4034 55820 None 55 Human Binding pAC50 = 4.4 4.4 - 1
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
CHEMBL1623 55820 None 55 Human Binding pAC50 = 4.4 4.4 - 1
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
DB00737 55820 None 55 Human Binding pAC50 = 4.4 4.4 - 1
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
5328940 100214 None 107 Human Binding pAC50 = 5.4 5.4 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
CHEMBL288441 100214 None 107 Human Binding pAC50 = 5.4 5.4 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
10531 1419 None 21 Human Binding pAC50 = 5.4 5.4 - 24
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
121 1419 None 21 Human Binding pAC50 = 5.4 5.4 - 24
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
888 1419 None 21 Human Binding pAC50 = 5.4 5.4 - 24
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
CHEMBL1732 1419 None 21 Human Binding pAC50 = 5.4 5.4 - 24
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
DB00320 1419 None 21 Human Binding pAC50 = 5.4 5.4 - 24
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
118422671 2755 None 65 Human Binding pAC50 = 5.3 5.3 - 4
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
1887 2755 None 65 Human Binding pAC50 = 5.3 5.3 - 4
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
189562 2755 None 65 Human Binding pAC50 = 5.3 5.3 - 4
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
71301 2755 None 65 Human Binding pAC50 = 5.3 5.3 - 4
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
7246 2755 None 65 Human Binding pAC50 = 5.3 5.3 - 4
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
9844194 2755 None 65 Human Binding pAC50 = 5.3 5.3 - 4
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL2365658 2755 None 65 Human Binding pAC50 = 5.3 5.3 - 4
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL3526436 2755 None 65 Human Binding pAC50 = 5.3 5.3 - 4
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL434394 2755 None 65 Human Binding pAC50 = 5.3 5.3 - 4
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
DB04861 2755 None 65 Human Binding pAC50 = 5.3 5.3 - 4
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
30323 62483 None 57 Human Binding pAC50 = 5.3 5.3 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL1563 62483 None 57 Human Binding pAC50 = 5.3 5.3 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL178 62483 None 57 Human Binding pAC50 = 5.3 5.3 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
10096344 89592 None 85 Human Binding pAC50 = 5.3 5.3 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 472 4 1 10 1.1 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(Cc1nc(C)c3ccccc3n1)c(=O)n2C 10.1038/s41467-023-40064-9
CHEMBL237500 89592 None 85 Human Binding pAC50 = 5.3 5.3 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 472 4 1 10 1.1 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(Cc1nc(C)c3ccccc3n1)c(=O)n2C 10.1038/s41467-023-40064-9
216416 111579 None 48 Human Binding pAC50 = 5.3 5.3 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL328190 111579 None 48 Human Binding pAC50 = 5.3 5.3 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
319 1323 None 44 Human Binding pAC50 = 5.3 5.3 - 9
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
321 1323 None 44 Human Binding pAC50 = 5.3 5.3 - 9
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
444031 1323 None 44 Human Binding pAC50 = 5.3 5.3 - 9
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
784 1323 None 44 Human Binding pAC50 = 5.3 5.3 - 9
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
CHEMBL1346 1323 None 44 Human Binding pAC50 = 5.3 5.3 - 9
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
DB00496 1323 None 44 Human Binding pAC50 = 5.3 5.3 - 9
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
3149 12612 None 15 Human Binding pAC50 = 5.2 5.2 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1187011 12612 None 15 Human Binding pAC50 = 5.2 5.2 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
4746 204889 None 31 Human Binding pAC50 = 5.2 5.2 - 4
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL1334033 204889 None 31 Human Binding pAC50 = 5.2 5.2 - 4
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL75880 204889 None 31 Human Binding pAC50 = 5.2 5.2 - 4
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
2335 11846 None 22 Human Binding pAC50 = 5.2 5.2 - 12
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
8478 11846 None 22 Human Binding pAC50 = 5.2 5.2 - 12
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 11846 None 22 Human Binding pAC50 = 5.2 5.2 - 12
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL221753 11846 None 22 Human Binding pAC50 = 5.2 5.2 - 12
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
65709 59879 None 39 Human Binding pAC50 = 5.2 5.2 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 365 8 0 5 3.3 CCN(CC)CCn1c(=O)c(Cc2ccc(OC)cc2)nc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1729803 59879 None 39 Human Binding pAC50 = 5.2 5.2 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 365 8 0 5 3.3 CCN(CC)CCn1c(=O)c(Cc2ccc(OC)cc2)nc2ccccc21 10.1038/s41467-023-40064-9
11643449 89953 None 3 Human Binding pAC50 = 5.2 5.2 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 753 6 5 10 2.7 CC[C@]1(O)C[C@@H]2CN(CCc3c([nH]c4ccccc34)[C@@](C(=O)OC)(c3cc4c(cc3OC)N(C)[C@H]3[C@@](O)(C(N)=O)[C@H](O)[C@]5(CC)C=CCN6CC[C@]43[C@@H]65)C2)C1 10.1038/s41467-023-40064-9
CHEMBL238071 89953 None 3 Human Binding pAC50 = 5.2 5.2 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 753 6 5 10 2.7 CC[C@]1(O)C[C@@H]2CN(CCc3c([nH]c4ccccc34)[C@@](C(=O)OC)(c3cc4c(cc3OC)N(C)[C@H]3[C@@](O)(C(N)=O)[C@H](O)[C@]5(CC)C=CCN6CC[C@]43[C@@H]65)C2)C1 10.1038/s41467-023-40064-9
2448 99321 None 70 Human Binding pAC50 = 5.2 5.2 - 18
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
CHEMBL28218 99321 None 70 Human Binding pAC50 = 5.2 5.2 - 18
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
DB12401 99321 None 70 Human Binding pAC50 = 5.2 5.2 - 18
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
4452 2760 None 19 Human Binding pAC50 = 5.2 5.2 - 19
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
983 2760 None 19 Human Binding pAC50 = 5.2 5.2 - 19
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
CHEMBL20734 2760 None 19 Human Binding pAC50 = 5.2 5.2 - 19
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
176 398 None 66 Human Binding pAC50 = 5.2 5.2 - 31
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2157 398 None 66 Human Binding pAC50 = 5.2 5.2 - 31
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2566 398 None 66 Human Binding pAC50 = 5.2 5.2 - 31
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
CHEMBL633 398 None 66 Human Binding pAC50 = 5.2 5.2 - 31
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
DB01118 398 None 66 Human Binding pAC50 = 5.2 5.2 - 31
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
1222 1662 None 49 Human Binding pAC50 = 5.2 5.2 - 33
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3396 1662 None 49 Human Binding pAC50 = 5.2 5.2 - 33
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
85 1662 None 49 Human Binding pAC50 = 5.2 5.2 - 33
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL46516 1662 None 49 Human Binding pAC50 = 5.2 5.2 - 33
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
DB04842 1662 None 49 Human Binding pAC50 = 5.2 5.2 - 33
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
5329102 194724 None 86 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 194724 None 86 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
72093 35059 None 9 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL1433361 35059 None 9 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL2103773 35059 None 9 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
42890 9423 None 59 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 497 3 5 10 1.0 CC(=O)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
CHEMBL1117 9423 None 59 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 497 3 5 10 1.0 CC(=O)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
1164 1628 None 26 Human Binding pAC50 = 5.1 5.1 - 12
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
1626 1628 None 26 Human Binding pAC50 = 5.1 5.1 - 12
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
3345 1628 None 26 Human Binding pAC50 = 5.1 5.1 - 12
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL596 1628 None 26 Human Binding pAC50 = 5.1 5.1 - 12
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
DB00813 1628 None 26 Human Binding pAC50 = 5.1 5.1 - 12
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
2247 505 None 81 Human Binding pAC50 = 5.1 5.1 - 42
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 505 None 81 Human Binding pAC50 = 5.1 5.1 - 42
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 505 None 81 Human Binding pAC50 = 5.1 5.1 - 42
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 505 None 81 Human Binding pAC50 = 5.1 5.1 - 42
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 505 None 81 Human Binding pAC50 = 5.1 5.1 - 42
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
5482 14418 None 80 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 386 6 0 4 5.9 Clc1ccc(C(Cn2ccnc2)OCc2ccsc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1200438 14418 None 80 Human Binding pAC50 = 5.1 5.1 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 386 6 0 4 5.9 Clc1ccc(C(Cn2ccnc2)OCc2ccsc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
1385580 29274 None 76 Human Binding pAC50 = 5.1 5.1 - 5
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
4615 29274 None 76 Human Binding pAC50 = 5.1 5.1 - 5
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL13828 29274 None 76 Human Binding pAC50 = 5.1 5.1 - 5
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
DB12877 29274 None 76 Human Binding pAC50 = 5.1 5.1 - 5
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
16722836 18983 None 99 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 524 10 3 8 4.8 Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1 10.1038/s41467-023-40064-9
CHEMBL1287853 18983 None 99 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 524 10 3 8 4.8 Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1 10.1038/s41467-023-40064-9
2794 19378 None 85 Human Binding pAC50 = 6.0 6.0 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 472 4 1 4 7.5 CC(C)/N=c1\cc2n(-c3ccc(Cl)cc3)c3ccccc3nc-2cc1Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1292 19378 None 85 Human Binding pAC50 = 6.0 6.0 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 472 4 1 4 7.5 CC(C)/N=c1\cc2n(-c3ccc(Cl)cc3)c3ccccc3nc-2cc1Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
3883 183533 None 112 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 369 5 1 4 3.5 Cc1c(OCC(F)(F)F)ccnc1C[S+]([O-])c1nc2ccccc2[nH]1 10.1038/s41467-023-40064-9
CHEMBL480 183533 None 112 Human Binding pAC50 = 5.0 5.0 - 0
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 369 5 1 4 3.5 Cc1c(OCC(F)(F)F)ccnc1C[S+]([O-])c1nc2ccccc2[nH]1 10.1038/s41467-023-40064-9
178024 1969 None 33 Human Binding pEC50 = 9.7 9.7 - 1
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 1969 None 33 Human Binding pEC50 = 9.7 9.7 - 1
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 1969 None 33 Human Binding pEC50 = 9.7 9.7 - 1
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 10313 None 0 Human Binding pEC50 = 9.2 9.2 - 0
Activity at human GHS-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 10313 None 0 Human Binding pEC50 = 9.2 9.2 - 0
Activity at human GHS-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 91831 None 0 Human Binding pEC50 = 9.2 9.2 - 0
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 91831 None 0 Human Binding pEC50 = 9.2 9.2 - 0
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 10313 None 0 Human Binding pEC50 = 9.2 9.2 - 0
Activity at human GHS-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 10313 None 0 Human Binding pEC50 = 9.2 9.2 - 0
Activity at human GHS-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 86000 None 0 Human Binding pEC50 = 9.1 9.1 - 0
Activity at human GHS-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 86000 None 0 Human Binding pEC50 = 9.1 9.1 - 0
Activity at human GHS-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 139273 None 0 Human Binding pEC50 = 9.1 9.1 - 0
Activity at human GHS-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 139273 None 0 Human Binding pEC50 = 9.1 9.1 - 0
Activity at human GHS-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 86000 None 0 Human Binding pEC50 = 9.1 9.1 - 0
Activity at human GHS-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 86000 None 0 Human Binding pEC50 = 9.1 9.1 - 0
Activity at human GHS-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 139273 None 0 Human Binding pEC50 = 9.1 9.1 - 0
Activity at human GHS-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 139273 None 0 Human Binding pEC50 = 9.1 9.1 - 0
Activity at human GHS-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 183015 None 5 Human Binding pEC50 = 9 9.0 - 0
Activity at human GHS-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 183015 None 5 Human Binding pEC50 = 9 9.0 - 0
Activity at human GHS-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 10307 None 0 Human Binding pEC50 = 9.0 9.0 - 0
Activity at human GHS-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 10307 None 0 Human Binding pEC50 = 9.0 9.0 - 0
Activity at human GHS-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 10307 None 0 Human Binding pEC50 = 9.0 9.0 - 0
Activity at human GHS-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 10307 None 0 Human Binding pEC50 = 9.0 9.0 - 0
Activity at human GHS-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 77876 None 0 Human Binding pEC50 = 8.9 8.9 - 0
Activity at human GHS-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 77876 None 0 Human Binding pEC50 = 8.9 8.9 - 0
Activity at human GHS-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 181521 None 0 Rat Binding pEC50 = 8.9 8.9 - 0
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 181521 None 0 Rat Binding pEC50 = 8.9 8.9 - 0
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 109298 None 0 Human Binding pEC50 = 8.9 8.9 - 0
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 109298 None 0 Human Binding pEC50 = 8.9 8.9 - 0
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 77876 None 0 Human Binding pEC50 = 8.9 8.9 - 0
Activity at human GHS-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 77876 None 0 Human Binding pEC50 = 8.9 8.9 - 0
Activity at human GHS-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 168152 None 0 Human Binding pEC50 = 8.8 8.8 - 0
Activity at human GHS-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 168152 None 0 Human Binding pEC50 = 8.8 8.8 - 0
Activity at human GHS-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 168152 None 0 Human Binding pEC50 = 8.8 8.8 - 0
Activity at human GHS-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 168152 None 0 Human Binding pEC50 = 8.8 8.8 - 0
Activity at human GHS-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 101223 None 0 Human Binding pEC50 = 8.7 8.7 - 0
Activity at human GHS-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 101223 None 0 Human Binding pEC50 = 8.7 8.7 - 0
Activity at human GHS-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 10304 None 0 Human Binding pEC50 = 8 8.0 - 0
Activity at human GHS-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 10304 None 0 Human Binding pEC50 = 8 8.0 - 0
Activity at human GHS-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 101086 None 0 Human Binding pEC50 = 8 8.0 - 0
Activity at human GHS-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 101086 None 0 Human Binding pEC50 = 8 8.0 - 0
Activity at human GHS-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 101086 None 0 Human Binding pEC50 = 8 8.0 - 0
Activity at human GHS-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 179382 None 0 Human Binding pEC50 = 7 7.0 - 0
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 179382 None 0 Human Binding pEC50 = 7 7.0 - 0
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 179382 None 0 Human Binding pEC50 = 7 7.0 - 0
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 179382 None 0 Human Binding pEC50 = 7 7.0 - 0
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 188366 None 0 Human Binding pEC50 = 6.9 6.9 - 0
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 188366 None 0 Human Binding pEC50 = 6.9 6.9 - 0
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 98268 None 0 Human Binding pEC50 = 7.9 7.9 - 0
Activity at human GHS-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 98268 None 0 Human Binding pEC50 = 7.9 7.9 - 0
Activity at human GHS-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 98268 None 0 Human Binding pEC50 = 7.9 7.9 - 0
Activity at human GHS-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 98268 None 0 Human Binding pEC50 = 7.9 7.9 - 0
Activity at human GHS-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 98268 None 0 Human Binding pEC50 = 7.9 7.9 - 0
Activity at human GHS-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 98268 None 0 Human Binding pEC50 = 7.9 7.9 - 0
Activity at human GHS-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 162767 None 0 Human Binding pEC50 = 7.8 7.8 - 0
Activity at human GHS-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 162767 None 0 Human Binding pEC50 = 7.8 7.8 - 0
Activity at human GHS-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 162767 None 0 Human Binding pEC50 = 7.8 7.8 - 0
Activity at human GHS-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 162767 None 0 Human Binding pEC50 = 7.8 7.8 - 0
Activity at human GHS-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 162767 None 0 Human Binding pEC50 = 7.8 7.8 - 0
Activity at human GHS-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 162767 None 0 Human Binding pEC50 = 7.8 7.8 - 0
Activity at human GHS-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 140118 None 0 Human Binding pEC50 = 7.8 7.8 - 0
Activity at human GHS-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 140118 None 0 Human Binding pEC50 = 7.8 7.8 - 0
Activity at human GHS-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 140118 None 0 Human Binding pEC50 = 7.7 7.7 - 0
Activity at human GHS-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 140118 None 0 Human Binding pEC50 = 7.7 7.7 - 0
Activity at human GHS-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 10306 None 0 Human Binding pEC50 = 8.7 8.7 - 0
Activity at human GHS-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 10306 None 0 Human Binding pEC50 = 8.7 8.7 - 0
Activity at human GHS-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 101223 None 0 Human Binding pEC50 = 8.7 8.7 - 0
Activity at human GHS-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 101223 None 0 Human Binding pEC50 = 8.7 8.7 - 0
Activity at human GHS-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 10303 None 1 Human Binding pEC50 = 8.7 8.7 - 0
Activity at human GHS-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 10303 None 1 Human Binding pEC50 = 8.7 8.7 - 0
Activity at human GHS-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 10303 None 1 Human Binding pEC50 = 8.7 8.7 - 0
Activity at human GHS-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 10303 None 1 Human Binding pEC50 = 8.7 8.7 - 0
Activity at human GHS-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 10306 None 0 Human Binding pEC50 = 8.6 8.6 - 0
Activity at human GHS-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 10306 None 0 Human Binding pEC50 = 8.6 8.6 - 0
Activity at human GHS-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 10308 None 0 Human Binding pEC50 = 8.6 8.6 - 0
Activity at human GHS-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 10308 None 0 Human Binding pEC50 = 8.6 8.6 - 0
Activity at human GHS-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 10308 None 0 Human Binding pEC50 = 8.6 8.6 - 0
Activity at human GHS-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 10308 None 0 Human Binding pEC50 = 8.6 8.6 - 0
Activity at human GHS-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 188184 None 0 Human Binding pEC50 = 7.7 7.7 - 0
Activity at human GHS-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 188184 None 0 Human Binding pEC50 = 7.7 7.7 - 0
Activity at human GHS-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 188184 None 0 Human Binding pEC50 = 7.7 7.7 - 0
Activity at human GHS-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 188184 None 0 Human Binding pEC50 = 7.7 7.7 - 0
Activity at human GHS-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 10407 None 0 Human Binding pEC50 = 8.5 8.5 - 0
Activity at human GHS-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 10407 None 0 Human Binding pEC50 = 8.5 8.5 - 0
Activity at human GHS-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 77742 None 2 Human Binding pEC50 = 8.5 8.5 - 0
Activity at human GHS-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 77742 None 2 Human Binding pEC50 = 8.5 8.5 - 0
Activity at human GHS-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 99247 None 17 Human Binding pEC50 = 8.5 8.5 - 0
Activity at human GHS-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 99247 None 17 Human Binding pEC50 = 8.5 8.5 - 0
Activity at human GHS-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 141208 None 0 Human Binding pEC50 = 8.5 8.5 - 0
Activity at human GHS-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 141208 None 0 Human Binding pEC50 = 8.5 8.5 - 0
Activity at human GHS-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 208926 None 0 Human Binding pEC50 = 8.5 8.5 - 0
Activity at human GHS-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 9725 None 33 Rat Binding pEC50 = 8.5 8.5 - 1
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 9725 None 33 Rat Binding pEC50 = 8.5 8.5 - 1
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 10407 None 0 Human Binding pEC50 = 8.5 8.5 - 0
Activity at human GHS-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 10407 None 0 Human Binding pEC50 = 8.5 8.5 - 0
Activity at human GHS-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 77742 None 2 Human Binding pEC50 = 8.5 8.5 - 0
Activity at human GHS-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 77742 None 2 Human Binding pEC50 = 8.5 8.5 - 0
Activity at human GHS-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 99247 None 17 Human Binding pEC50 = 8.5 8.5 - 0
Activity at human GHS-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 99247 None 17 Human Binding pEC50 = 8.5 8.5 - 0
Activity at human GHS-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 141208 None 0 Human Binding pEC50 = 8.5 8.5 - 0
Activity at human GHS-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 141208 None 0 Human Binding pEC50 = 8.5 8.5 - 0
Activity at human GHS-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 208926 None 0 Human Binding pEC50 = 8.5 8.5 - 0
Activity at human GHS-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 77259 None 1 Human Binding pEC50 = 8.4 8.4 - 0
Activity at human GHS-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 77259 None 1 Human Binding pEC50 = 8.4 8.4 - 0
Activity at human GHS-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 77259 None 1 Human Binding pEC50 = 8.4 8.4 - 0
Activity at human GHS-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 77259 None 1 Human Binding pEC50 = 8.4 8.4 - 0
Activity at human GHS-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 10301 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 10301 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 10301 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 10301 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 10312 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 10312 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 138187 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 138187 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 139534 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 139534 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 169282 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 169282 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 10312 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 10312 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 138187 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 138187 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 139534 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 139534 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 169282 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 169282 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 10302 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 10302 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 10302 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 10302 None 0 Human Binding pEC50 = 8.3 8.3 - 0
Activity at human GHS-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 102189 None 0 Rat Binding pEC50 = 7.3 7.3 - 0
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 102189 None 0 Rat Binding pEC50 = 7.3 7.3 - 0
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 183609 None 0 Human Binding pEC50 = 6.3 6.3 - 0
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 183609 None 0 Human Binding pEC50 = 6.3 6.3 - 0
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 10311 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Activity at human GHS-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 10311 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Activity at human GHS-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 10311 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Activity at human GHS-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 10311 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Activity at human GHS-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 10310 None 0 Human Binding pEC50 = 8.2 8.2 - 0
Activity at human GHS-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 10310 None 0 Human Binding pEC50 = 8.2 8.2 - 0
Activity at human GHS-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 101239 None 0 Human Binding pEC50 = 8.2 8.2 - 0
Activity at human GHS-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 101239 None 0 Human Binding pEC50 = 8.2 8.2 - 0
Activity at human GHS-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 10310 None 0 Human Binding pEC50 = 8.2 8.2 - 0
Activity at human GHS-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 10310 None 0 Human Binding pEC50 = 8.2 8.2 - 0
Activity at human GHS-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 101239 None 0 Human Binding pEC50 = 8.2 8.2 - 0
Activity at human GHS-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 101239 None 0 Human Binding pEC50 = 8.2 8.2 - 0
Activity at human GHS-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 141334 None 0 Human Binding pEC50 = 8.1 8.1 - 0
Activity at human GHS-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 141334 None 0 Human Binding pEC50 = 8.1 8.1 - 0
Activity at human GHS-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 141334 None 0 Human Binding pEC50 = 8.1 8.1 - 0
Activity at human GHS-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 141334 None 0 Human Binding pEC50 = 8.1 8.1 - 0
Activity at human GHS-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 211562 None 0 Human Binding pEC50 = 7.1 7.1 - 0
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 10305 None 0 Human Binding pEC50 = 8.1 8.1 - 0
Activity at human GHS-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 10305 None 0 Human Binding pEC50 = 8.1 8.1 - 0
Activity at human GHS-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 10309 None 0 Human Binding pEC50 = 8.1 8.1 - 0
Activity at human GHS-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 10309 None 0 Human Binding pEC50 = 8.1 8.1 - 0
Activity at human GHS-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 10305 None 0 Human Binding pEC50 = 8.1 8.1 - 0
Activity at human GHS-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 10305 None 0 Human Binding pEC50 = 8.1 8.1 - 0
Activity at human GHS-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 10309 None 0 Human Binding pEC50 = 8.1 8.1 - 0
Activity at human GHS-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 10309 None 0 Human Binding pEC50 = 8.1 8.1 - 0
Activity at human GHS-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 62913 None 0 Human Binding pIC50 = 10.7 10.7 - 0
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 62913 None 0 Human Binding pIC50 = 10.7 10.7 - 0
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 113441 None 0 Human Binding pIC50 = 10.1 10.1 - 0
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 113441 None 0 Human Binding pIC50 = 10.1 10.1 - 0
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 214131 None 0 Human Binding pIC50 = 10.1 10.1 - 0
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 193414 None 0 Human Binding pIC50 = 9.9 9.9 - 0
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 193414 None 0 Human Binding pIC50 = 9.9 9.9 - 0
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 193414 None 0 Human Binding pIC50 = 9.9 9.9 - 0
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 209493 None 0 Human Binding pIC50 = 9.9 9.9 - 0
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 109270 None 0 Human Binding pIC50 = 9.9 9.9 - 0
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 109270 None 0 Human Binding pIC50 = 9.9 9.9 - 0
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 214113 None 0 Human Binding pIC50 = 9.9 9.9 - 1
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 113445 None 0 Human Binding pIC50 = 9.8 9.8 - 0
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 113445 None 0 Human Binding pIC50 = 9.8 9.8 - 0
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 209491 None 0 Human Binding pIC50 = 9.8 9.8 - 0
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 141333 None 0 Human Binding pIC50 = 9.7 9.7 - 0
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 141333 None 0 Human Binding pIC50 = 9.7 9.7 - 0
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 108568 None 0 Human Binding pIC50 = 9.7 9.7 - 0
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 108568 None 0 Human Binding pIC50 = 9.7 9.7 - 0
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 121586 None 0 Human Binding pIC50 = 9.6 9.6 - 0
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 121586 None 0 Human Binding pIC50 = 9.6 9.6 - 0
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 113470 None 0 Human Binding pIC50 = 9.6 9.6 - 0
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 113470 None 0 Human Binding pIC50 = 9.6 9.6 - 0
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 63865 None 0 Human Binding pIC50 = 9.6 9.6 - 0
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 63865 None 0 Human Binding pIC50 = 9.6 9.6 - 0
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 213329 None 18 Human Binding pIC50 = 9.6 9.6 - 1
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 213329 None 18 Human Binding pIC50 = 9.6 9.6 - 1
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 214113 None 0 Human Binding pIC50 = 9.6 9.6 - 1
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 109272 None 0 Human Binding pIC50 = 9.6 9.6 - 0
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 109272 None 0 Human Binding pIC50 = 9.6 9.6 - 0
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 122007 None 0 Rat Binding pIC50 = 9.6 9.6 - 0
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 122007 None 0 Rat Binding pIC50 = 9.6 9.6 - 0
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 113446 None 0 Human Binding pIC50 = 9.5 9.5 - 0
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 113446 None 0 Human Binding pIC50 = 9.5 9.5 - 0
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 96932 None 0 Human Binding pIC50 = 9.5 9.5 - 0
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 96932 None 0 Human Binding pIC50 = 9.5 9.5 - 0
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 96932 None 0 Human Binding pIC50 = 9.5 9.5 - 0
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 96932 None 0 Human Binding pIC50 = 9.5 9.5 - 0
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 166035 None 0 Human Binding pIC50 = 9.5 9.5 - 0
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 166035 None 0 Human Binding pIC50 = 9.5 9.5 - 0
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 122000 None 0 Human Binding pIC50 = 9.5 9.5 - 0
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 122000 None 0 Human Binding pIC50 = 9.5 9.5 - 0
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 166035 None 0 Human Binding pIC50 = 9.5 9.5 - 0
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 166035 None 0 Human Binding pIC50 = 9.5 9.5 - 0
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 113444 None 0 Human Binding pIC50 = 9.5 9.5 - 0
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 113444 None 0 Human Binding pIC50 = 9.5 9.5 - 0
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 113469 None 0 Human Binding pIC50 = 9.5 9.5 - 0
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 113469 None 0 Human Binding pIC50 = 9.5 9.5 - 0
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 113443 None 0 Human Binding pIC50 = 9.5 9.5 - 0
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 113443 None 0 Human Binding pIC50 = 9.5 9.5 - 0
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 214113 None 0 Human Binding pIC50 = 9.4 9.4 - 1
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 121996 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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 121996 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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 113480 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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 113480 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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 1969 None 33 Human Binding pIC50 = 9.4 9.4 - 1
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 1969 None 33 Human Binding pIC50 = 9.4 9.4 - 1
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 1969 None 33 Human Binding pIC50 = 9.4 9.4 - 1
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 77342 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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 77342 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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 138533 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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 138533 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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 188720 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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 188720 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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 188720 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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 121999 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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 121999 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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 113473 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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 113473 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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 122007 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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 122007 None 0 Human Binding pIC50 = 9.4 9.4 - 0
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 113452 None 0 Human Binding pIC50 = 9.3 9.3 - 0
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 113452 None 0 Human Binding pIC50 = 9.3 9.3 - 0
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 79158 None 1 Human Binding pIC50 = 9.3 9.3 - 0
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 79158 None 1 Human Binding pIC50 = 9.3 9.3 - 0
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 1969 None 33 Human Binding pIC50 = 9.3 9.3 - 1
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 1969 None 33 Human Binding pIC50 = 9.3 9.3 - 1
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 1969 None 33 Human Binding pIC50 = 9.3 9.3 - 1
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 113451 None 0 Human Binding pIC50 = 9.3 9.3 - 0
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 113451 None 0 Human Binding pIC50 = 9.3 9.3 - 0
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 113471 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 113471 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 125190 None 0 Human Binding pIC50 = 9.2 9.2 - 1
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 125190 None 0 Human Binding pIC50 = 9.2 9.2 - 1
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 96932 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 96932 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 91547 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 91547 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 113468 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 113468 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 1969 None 33 Human Binding pIC50 = 9.2 9.2 - 1
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 1969 None 33 Human Binding pIC50 = 9.2 9.2 - 1
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 1969 None 33 Human Binding pIC50 = 9.2 9.2 - 1
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 113449 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 113449 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 113448 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 113448 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 121332 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 121332 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 154786 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 154786 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 213729 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 1969 None 33 Human Binding pIC50 = 9.1 9.1 - 1
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 1969 None 33 Human Binding pIC50 = 9.1 9.1 - 1
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 1969 None 33 Human Binding pIC50 = 9.1 9.1 - 1
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 213023 None 0 Human Binding pIC50 = 9.1 9.1 - 0
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 113447 None 18 Human Binding pIC50 = 9.1 9.1 - 0
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 113447 None 18 Human Binding pIC50 = 9.1 9.1 - 0
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 75986 None 0 Human Binding pIC50 = 9.1 9.1 - 0
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 75986 None 0 Human Binding pIC50 = 9.1 9.1 - 0
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 215695 None 0 Human Binding pIC50 = 9.1 9.1 - 0
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 145654 None 0 Human Binding pIC50 = 9.1 9.1 - 0
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 145654 None 0 Human Binding pIC50 = 9.1 9.1 - 0
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 109320 None 0 Human Binding pIC50 = 9.0 9.0 - 0
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 109320 None 0 Human Binding pIC50 = 9.0 9.0 - 0
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 113479 None 0 Human Binding pIC50 = 9.0 9.0 - 0
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 113479 None 0 Human Binding pIC50 = 9.0 9.0 - 0
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 209490 None 0 Human Binding pIC50 = 9.0 9.0 - 0
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 121585 None 0 Human Binding pIC50 = 9.0 9.0 - 0
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 121585 None 0 Human Binding pIC50 = 9.0 9.0 - 0
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 121996 None 0 Rat Binding pIC50 = 9.0 9.0 - 0
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 121996 None 0 Rat Binding pIC50 = 9.0 9.0 - 0
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 209492 None 0 Human Binding pIC50 = 9.0 9.0 - 0
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 75507 None 0 Human Binding pIC50 = 9 9.0 - 0
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 75507 None 0 Human Binding pIC50 = 9 9.0 - 0
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 94401 None 0 Human Binding pIC50 = 9.0 9.0 - 0
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 94401 None 0 Human Binding pIC50 = 9.0 9.0 - 0
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 109275 None 0 Human Binding pIC50 = 9.0 9.0 - 0
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 109275 None 0 Human Binding pIC50 = 9.0 9.0 - 0
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 109276 None 0 Human Binding pIC50 = 9.0 9.0 - 0
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 109276 None 0 Human Binding pIC50 = 9.0 9.0 - 0
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 99429 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 99429 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 3622 None 4 Human Binding pIC50 = 8.9 8.9 - 0
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 3622 None 4 Human Binding pIC50 = 8.9 8.9 - 0
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 3622 None 4 Human Binding pIC50 = 8.9 8.9 - 0
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 75991 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 75991 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 125191 None 0 Human Binding pIC50 = 8.9 8.9 - 1
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 125191 None 0 Human Binding pIC50 = 8.9 8.9 - 1
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 113439 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 113439 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 113453 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 113453 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 125195 None 0 Human Binding pIC50 = 8.9 8.9 - 1
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 125195 None 0 Human Binding pIC50 = 8.9 8.9 - 1
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 109271 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 109271 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 76005 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 76005 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 76765 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 76765 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 109293 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 109293 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 109312 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 109312 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 123554 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 123554 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 109298 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 109298 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 109308 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 109308 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 154640 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 154640 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 109294 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 109294 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 94182 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 94182 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 94619 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 94619 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 1969 None 33 Human Binding pIC50 = 8.7 8.7 - 1
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 1969 None 33 Human Binding pIC50 = 8.7 8.7 - 1
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 1969 None 33 Human Binding pIC50 = 8.7 8.7 - 1
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 92012 None 0 Human Binding pIC50 = 8 8.0 - 0
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 92012 None 0 Human Binding pIC50 = 8 8.0 - 0
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 77141 None 0 Human Binding pIC50 = 8 8.0 - 0
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 77141 None 0 Human Binding pIC50 = 8 8.0 - 0
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 121350 None 0 Human Binding pIC50 = 7 7.0 - 0
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 121350 None 0 Human Binding pIC50 = 7 7.0 - 0
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 84719 None 0 Human Binding pIC50 = 7 7.0 - 0
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 84719 None 0 Human Binding pIC50 = 7 7.0 - 0
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 178125 None 0 Human Binding pIC50 = 7 7.0 - 0
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 178125 None 0 Human Binding pIC50 = 7 7.0 - 0
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 162283 None 0 Human Binding pIC50 = 7 7.0 - 0
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 162283 None 0 Human Binding pIC50 = 7 7.0 - 0
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 162513 None 0 Human Binding pIC50 = 7 7.0 - 0
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 162513 None 0 Human Binding pIC50 = 7 7.0 - 0
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 137233 None 0 Human Binding pIC50 = 6 6.0 - 0
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 137233 None 0 Human Binding pIC50 = 6 6.0 - 0
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 162264 None 0 Human Binding pIC50 = 6 6.0 - 0
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 162264 None 0 Human Binding pIC50 = 6 6.0 - 0
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 177653 None 0 Human Binding pIC50 = 5 5.0 - 0
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 177653 None 0 Human Binding pIC50 = 5 5.0 - 0
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 179529 None 0 Human Binding pIC50 = 4 4.0 - 0
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 179529 None 0 Human Binding pIC50 = 4 4.0 - 0
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 75872 None 0 Human Binding pIC50 = 7.0 7.0 - 1
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 75872 None 0 Human Binding pIC50 = 7.0 7.0 - 1
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 209489 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 178125 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 178125 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 94183 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 94183 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 64077 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 64077 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 162283 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 162283 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 75870 None 0 Human Binding pIC50 = 6.0 6.0 - 1
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 75870 None 0 Human Binding pIC50 = 6.0 6.0 - 1
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 154639 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 154639 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 141798 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 141798 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 141798 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 141798 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 5952 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 5952 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 92273 None 0 Human Binding pIC50 = 6.0 6.0 - 1
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 92273 None 0 Human Binding pIC50 = 6.0 6.0 - 1
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 130453 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 130453 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 209495 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 121576 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 121576 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 94181 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 94181 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 84934 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 84934 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 137674 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 137674 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 109322 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 109322 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 137674 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 137674 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 146937 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 146937 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 76638 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 76638 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 76023 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 76023 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 122007 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
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 122007 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
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 154676 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 154676 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 66160 None 1 Human Binding pIC50 = 7.0 7.0 - 0
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 66160 None 1 Human Binding pIC50 = 7.0 7.0 - 0
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 84333 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 84333 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 75525 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 75525 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 121579 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
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 121579 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
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 7925 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 7925 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 154677 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 154677 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 81599 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 81599 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 91762 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 91762 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 162718 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 162718 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 64414 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 64414 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 81604 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 81604 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 209919 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 137034 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 137034 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 109277 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 109277 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 109313 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 109313 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 137034 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 137034 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 214118 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 126765 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
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 126765 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
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 92269 None 0 Human Binding pIC50 = 7.9 7.9 - 1
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 92269 None 0 Human Binding pIC50 = 7.9 7.9 - 1
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 162277 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 162277 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 162660 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 162660 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 162691 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 162691 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 162774 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 162774 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 160310 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 160310 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 166728 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 166728 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 85135 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 85135 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 109303 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 109303 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 109309 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 109309 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 75876 None 0 Human Binding pIC50 = 6.9 6.9 - 1
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 75876 None 0 Human Binding pIC50 = 6.9 6.9 - 1
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 84679 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 84679 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 113459 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 113459 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 409 3 2 6 3.3 CS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL499371 214093 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 81614 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 81614 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 81614 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 81614 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 122030 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 122030 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 84679 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 84679 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 67113 None 1 Human Binding pIC50 = 6.9 6.9 - 0
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 67113 None 1 Human Binding pIC50 = 6.9 6.9 - 0
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 99151 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 99151 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 121334 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 121334 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 75506 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 75506 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 2451 None 20 Human Binding pIC50 = 6.9 6.9 - 0
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 2451 None 20 Human Binding pIC50 = 6.9 6.9 - 0
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 2451 None 20 Human Binding pIC50 = 6.9 6.9 - 0
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 2451 None 20 Human Binding pIC50 = 6.9 6.9 - 0
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 84935 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 84935 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 211764 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 162484 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 162484 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 211764 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 78501 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 78501 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 162484 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 162484 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 11273 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 11273 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 11273 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 5770 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 5770 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 79156 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 79156 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 75553 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 75553 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 113436 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 113436 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 5626 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 5626 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 214220 None 0 Human Binding pIC50 = 7.9 7.9 - 1
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 214220 None 0 Human Binding pIC50 = 7.9 7.9 - 1
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 162774 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 162774 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 213640 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 62996 None 17 Human Binding pIC50 = 6.9 6.9 - 0
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 62996 None 17 Human Binding pIC50 = 6.9 6.9 - 0
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 62996 None 17 Human Binding pIC50 = 6.9 6.9 - 0
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 62996 None 17 Human Binding pIC50 = 6.9 6.9 - 0
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 121337 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 121337 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 137192 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 137192 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 161786 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 161786 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 170031 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 170031 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 62996 None 17 Human Binding pIC50 = 6.9 6.9 - 0
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 62996 None 17 Human Binding pIC50 = 6.9 6.9 - 0
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 178165 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 178165 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 94554 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 94554 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 123856 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 123856 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 109137 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 109137 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 67075 None 1 Human Binding pIC50 = 6.9 6.9 - 0
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 67075 None 1 Human Binding pIC50 = 6.9 6.9 - 0
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 65202 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 65202 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 148764 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 148764 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 81617 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 81617 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 81617 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 81617 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 148309 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 148309 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 5778 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 5778 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 66184 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 66184 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 154938 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 154938 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 137221 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 137221 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 75873 None 0 Human Binding pIC50 = 7.9 7.9 - 1
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 75873 None 0 Human Binding pIC50 = 7.9 7.9 - 1
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 162277 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 162277 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 162660 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 162660 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 162691 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 162691 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 5807 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 5807 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 177911 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 177911 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 154904 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 154904 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 137107 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 137107 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 137191 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 137191 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 141938 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 141938 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 155415 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 155415 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 121576 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
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 121576 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
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 12796 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 12796 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 12796 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 84695 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 84695 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 124379 None 2 Human Binding pIC50 = 6.8 6.8 - 0
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 124379 None 2 Human Binding pIC50 = 6.8 6.8 - 0
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 188861 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 188861 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 188861 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 188861 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 136717 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 136717 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 109304 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 109304 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 136717 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 136717 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 113476 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 113476 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 177296 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 177296 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 63642 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 63642 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 92268 None 0 Human Binding pIC50 = 7.8 7.8 - 1
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 92268 None 0 Human Binding pIC50 = 7.8 7.8 - 1
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 177296 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 177296 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 177579 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 177579 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 177911 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 177911 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 162722 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 162722 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 1606 None 45 Human Binding pIC50 = 7.8 7.8 - 1
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 1606 None 45 Human Binding pIC50 = 7.8 7.8 - 1
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 1606 None 45 Human Binding pIC50 = 7.8 7.8 - 1
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 66911 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 66911 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 121574 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 121574 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 121302 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 121302 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 84331 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 84331 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 138135 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 138135 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 168375 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 168375 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 6539 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 6539 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 138397 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 138397 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 148166 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 148166 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 81620 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 81620 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 81620 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 81620 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 13094 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 13094 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 13094 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 64458 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 64458 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 109273 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 109273 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 92013 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 92013 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 162722 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 162722 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 77882 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 77882 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 76257 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 76257 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 5826 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 5826 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 99151 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 99151 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 125197 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 125197 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 98348 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 98348 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 94184 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 94184 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 75377 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 75377 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 66101 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 66101 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 109747 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 109747 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 5781 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 5781 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 175032 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 175032 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 81608 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 81608 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 66330 None 1 Human Binding pIC50 = 6.8 6.8 - 0
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 66330 None 1 Human Binding pIC50 = 6.8 6.8 - 0
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 98348 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 98348 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 174308 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 174308 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 81612 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 81612 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 5706 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 5706 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 67338 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 67338 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 77710 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 77710 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 177579 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 177579 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 168397 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 168397 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 121577 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
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 121577 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
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 136637 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 136637 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 5762 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 5762 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 150489 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 150489 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 155389 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 155389 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 166767 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 166767 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 161896 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 161896 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 90957 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 90957 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 99148 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 99148 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 66338 None 1 Human Binding pIC50 = 7.8 7.8 - 0
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 66338 None 1 Human Binding pIC50 = 7.8 7.8 - 0
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 1606 None 45 Human Binding pIC50 = 7.8 7.8 - 1
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 1606 None 45 Human Binding pIC50 = 7.8 7.8 - 1
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 1606 None 45 Human Binding pIC50 = 7.8 7.8 - 1
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 137877 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 137877 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 137877 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 137877 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 146151 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 146151 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 153055 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 153055 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 139296 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 139296 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 154817 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 154817 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 121578 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 121578 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 162087 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 162087 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 98386 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 98386 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 64020 None 0 Human Binding pIC50 = 4.7 4.7 - 0
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 64020 None 0 Human Binding pIC50 = 4.7 4.7 - 0
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 75394 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 75394 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 162255 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 162255 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 162053 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 162053 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 162283 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 162283 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 79162 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 79162 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 165924 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 165924 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 165924 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 165924 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 76742 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 76742 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 177940 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 177940 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 9725 None 33 Human Binding pIC50 = 7.7 7.7 - 1
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 9725 None 33 Human Binding pIC50 = 7.7 7.7 - 1
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 109318 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 109318 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 79150 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 79150 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 120340 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 120340 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 177190 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 177190 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 62503 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 62503 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 140557 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 140557 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 124030 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 124030 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 84738 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 84738 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 81616 None 0 Human Binding pIC50 = 4.7 4.7 - 0
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 81616 None 0 Human Binding pIC50 = 4.7 4.7 - 0
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 81616 None 0 Human Binding pIC50 = 4.7 4.7 - 0
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 81616 None 0 Human Binding pIC50 = 4.7 4.7 - 0
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 75864 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 75864 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 162053 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 162053 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 162087 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 162087 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 162255 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 162255 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 162283 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 162283 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 144040 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 144040 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 121340 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 121340 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 121344 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 121344 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 1969 None 33 Human Binding pIC50 = 8.7 8.7 - 1
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 1969 None 33 Human Binding pIC50 = 8.7 8.7 - 1
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 1969 None 33 Human Binding pIC50 = 8.7 8.7 - 1
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 76035 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 76035 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 5828 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 5828 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 121997 None 0 Rat Binding pIC50 = 8.7 8.7 - 0
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 121997 None 0 Rat Binding pIC50 = 8.7 8.7 - 0
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 3622 None 4 Human Binding pIC50 = 8.7 8.7 - 0
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 3622 None 4 Human Binding pIC50 = 8.7 8.7 - 0
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 3622 None 4 Human Binding pIC50 = 8.7 8.7 - 0
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 214113 None 0 Human Binding pIC50 = 8.6 8.6 - 1
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 214113 None 0 Human Binding pIC50 = 8.6 8.6 - 1
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 76704 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 76704 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 141317 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 141317 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 109310 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 109310 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 140485 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 140485 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 76027 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 76027 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 75983 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 75983 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 75985 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 75985 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 113475 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 113475 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 98970 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 98970 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 13968 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 13968 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 13968 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 109314 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 109314 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 169004 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 169004 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 76830 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 76830 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 121581 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
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 121581 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
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 75882 None 0 Human Binding pIC50 = 6.7 6.7 - 1
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 75882 None 0 Human Binding pIC50 = 6.7 6.7 - 1
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 12032 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 12032 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 12032 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 65229 None 1 Human Binding pIC50 = 7.7 7.7 - 0
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 65229 None 1 Human Binding pIC50 = 7.7 7.7 - 0
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 141609 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 141609 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 75370 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 75370 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 75966 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 75966 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 177940 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 177940 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 5827 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 5827 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 162718 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 162718 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 113457 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 113457 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 214431 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 178213 None 0 Human Binding pIC50 = 4.7 4.7 - 0
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 178213 None 0 Human Binding pIC50 = 4.7 4.7 - 0
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 75865 None 0 Human Binding pIC50 = 6.7 6.7 - 1
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 75865 None 0 Human Binding pIC50 = 6.7 6.7 - 1
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 98247 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 98247 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 75865 None 0 Human Binding pIC50 = 6.7 6.7 - 1
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 75865 None 0 Human Binding pIC50 = 6.7 6.7 - 1
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 138014 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 138014 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 9725 None 33 Human Binding pIC50 = 7.7 7.7 - 1
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 9725 None 33 Human Binding pIC50 = 7.7 7.7 - 1
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 99218 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 99218 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 2451 None 20 Human Binding pIC50 = 7.6 7.6 - 0
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 2451 None 20 Human Binding pIC50 = 7.6 7.6 - 0
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 2451 None 20 Human Binding pIC50 = 7.6 7.6 - 0
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 2451 None 20 Human Binding pIC50 = 7.6 7.6 - 0
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 121333 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 121333 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 154979 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 154979 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 137190 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 137190 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 137592 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 137592 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 64871 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 64871 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 141810 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 141810 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 79722 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 79722 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 68805 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 68805 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 109301 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 109301 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 147185 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 147185 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 113464 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 113464 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 75867 None 0 Human Binding pIC50 = 6.6 6.6 - 1
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 75867 None 0 Human Binding pIC50 = 6.6 6.6 - 1
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 121579 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 121579 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 79159 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 79159 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 121346 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 121346 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 121349 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 121349 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 84673 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 84673 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 163022 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 163022 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 5740 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 5740 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 76178 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 76178 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 162499 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 162499 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 76740 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 76740 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 177906 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 177906 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 124386 None 1 Human Binding pIC50 = 7.6 7.6 - 0
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 124386 None 1 Human Binding pIC50 = 7.6 7.6 - 0
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 180207 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 180207 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 75878 None 0 Human Binding pIC50 = 7.6 7.6 - 1
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 75878 None 0 Human Binding pIC50 = 7.6 7.6 - 1
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 98440 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 98440 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 121336 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 121336 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2Br)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3586019 211799 None 6 Rat Binding pIC50 = 6.6 6.6 - 0
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 121584 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
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 121584 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
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 177906 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 177906 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 162499 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 162499 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 163022 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 163022 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 91586 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 91586 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 122006 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
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 122006 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
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 121575 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 121575 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 5759 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 5759 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 11260 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 11260 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 11260 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 109323 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 109323 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 113462 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 113462 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 188835 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 188835 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 188835 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 188835 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 154674 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 154674 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 65566 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 65566 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 177308 None 0 Human Binding pIC50 = 4.6 4.6 - 0
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 177308 None 0 Human Binding pIC50 = 4.6 4.6 - 0
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 5670 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 5670 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 147305 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 147305 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 77051 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 77051 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 81615 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 81615 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 81615 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 81615 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 76256 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 76256 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 137222 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 137222 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 79152 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 79152 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 5816 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 5816 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 121997 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
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 121997 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
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 2232 None 24 Human Binding pIC50 = 5.6 5.6 - 1
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 2232 None 24 Human Binding pIC50 = 5.6 5.6 - 1
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 2232 None 24 Human Binding pIC50 = 5.6 5.6 - 1
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 209919 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 162727 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 162727 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 67010 None 1 Human Binding pIC50 = 7.5 7.5 - 0
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 67010 None 1 Human Binding pIC50 = 7.5 7.5 - 0
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 161867 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 161867 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 79157 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 79157 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 162585 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 162585 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 177333 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 177333 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 98440 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 98440 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 75995 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 75995 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 75880 None 0 Human Binding pIC50 = 6.5 6.5 - 1
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 75880 None 0 Human Binding pIC50 = 6.5 6.5 - 1
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 75866 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 75866 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 125193 None 0 Human Binding pIC50 = 8.5 8.5 - 1
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 125193 None 0 Human Binding pIC50 = 8.5 8.5 - 1
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 121339 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 121339 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 154673 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 154673 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 122006 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 122006 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 125196 None 0 Human Binding pIC50 = 8.5 8.5 - 1
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 125196 None 0 Human Binding pIC50 = 8.5 8.5 - 1
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 214133 None 23 Human Binding pIC50 = 8.5 8.5 - 1
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 125192 None 0 Human Binding pIC50 = 8.5 8.5 - 1
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 125192 None 0 Human Binding pIC50 = 8.5 8.5 - 1
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 125194 None 0 Human Binding pIC50 = 8.5 8.5 - 1
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 125194 None 0 Human Binding pIC50 = 8.5 8.5 - 1
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 121343 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 121343 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 76748 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 76748 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 208466 None 38 Human Binding pIC50 = 8.4 8.4 - 1
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 76670 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 76670 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 113474 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 113474 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 1872 None 8 Human Binding pIC50 = 8.4 8.4 - 0
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 1872 None 8 Human Binding pIC50 = 8.4 8.4 - 0
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 1872 None 8 Human Binding pIC50 = 8.4 8.4 - 0
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 177487 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 177487 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 162299 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 162299 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 5822 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 5822 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 92275 None 0 Human Binding pIC50 = 7.5 7.5 - 1
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 92275 None 0 Human Binding pIC50 = 7.5 7.5 - 1
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 1969 None 33 Human Binding pIC50 = 6.5 6.5 - 1
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 1969 None 33 Human Binding pIC50 = 6.5 6.5 - 1
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 1969 None 33 Human Binding pIC50 = 6.5 6.5 - 1
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 161898 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 161898 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 136282 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 136282 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 76533 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 76533 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 9725 None 33 Human Binding pIC50 = 5.5 5.5 - 1
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 9725 None 33 Human Binding pIC50 = 5.5 5.5 - 1
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 138933 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 138933 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 177333 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 177333 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 162585 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 162585 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 162932 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 162932 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 84426 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 84426 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 140844 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 140844 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 140844 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 140844 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 5953 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 5953 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 162061 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 162061 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 162727 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 162727 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 76199 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 76199 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 126765 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 126765 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 1969 None 33 Human Binding pIC50 = 7.5 7.5 - 1
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 1969 None 33 Human Binding pIC50 = 7.5 7.5 - 1
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 1969 None 33 Human Binding pIC50 = 7.5 7.5 - 1
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 154895 None 24 Human Binding pIC50 = 7.5 7.5 - 1
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 154895 None 24 Human Binding pIC50 = 7.5 7.5 - 1
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 109295 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 109295 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 146427 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 146427 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 152476 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 152476 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 154895 None 24 Human Binding pIC50 = 7.5 7.5 - 1
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 154895 None 24 Human Binding pIC50 = 7.5 7.5 - 1
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 122000 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
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 122000 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
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 75883 None 0 Human Binding pIC50 = 6.5 6.5 - 1
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 75883 None 0 Human Binding pIC50 = 6.5 6.5 - 1
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 209323 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 209323 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 75064 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 75064 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 154641 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 154641 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 137234 None 1 Human Binding pIC50 = 7.5 7.5 - 0
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 137234 None 1 Human Binding pIC50 = 7.5 7.5 - 0
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 113477 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 113477 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 99148 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 99148 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 125056 None 1 Human Binding pIC50 = 7.5 7.5 - 0
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 125056 None 1 Human Binding pIC50 = 7.5 7.5 - 0
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 155012 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 155012 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 12922 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 12922 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 12922 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 13093 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 13093 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 13093 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 62597 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 62597 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 162061 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 162061 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 161953 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 161953 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 162932 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 162932 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 79154 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 79154 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 64574 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 64574 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 121582 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
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 121582 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
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 13058 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 13058 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 13058 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 167841 None 0 Human Binding pIC50 = 4.5 4.5 - 0
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 167841 None 0 Human Binding pIC50 = 4.5 4.5 - 0
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 167896 None 0 Human Binding pIC50 = 4.5 4.5 - 0
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 167896 None 0 Human Binding pIC50 = 4.5 4.5 - 0
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 75884 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 75884 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 121577 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 121577 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 122006 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
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 122006 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
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 12049 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 12049 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 12049 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 81602 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 81602 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 177121 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 177121 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 80215 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 80215 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 168336 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 168336 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 75788 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 75788 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 92272 None 0 Human Binding pIC50 = 7.4 7.4 - 1
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 92272 None 0 Human Binding pIC50 = 7.4 7.4 - 1
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 109300 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 109300 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 64612 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 64612 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 81618 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 81618 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 81618 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 81618 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 90647 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 90647 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 116196 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 116196 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 148311 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 148311 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 141215 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 141215 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 121338 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 121338 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 68805 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 68805 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 81601 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 81601 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 127171 None 1 Human Binding pIC50 = 6.4 6.4 - 0
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 127171 None 1 Human Binding pIC50 = 6.4 6.4 - 0
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 66668 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 66668 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 126823 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 126823 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 99218 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 99218 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 193399 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 193399 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 193399 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 193399 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 177121 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 177121 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 178221 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 178221 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 121580 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
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 121580 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
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 99429 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 99429 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 138817 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 138817 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 98247 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 98247 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 163001 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 163001 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 121342 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 121342 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 177487 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 177487 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 162299 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 162299 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 139240 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 139240 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 131990 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 131990 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 75497 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 75497 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 121586 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
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 121586 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
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 76722 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 76722 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 113440 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 113440 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 64840 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 64840 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 75879 None 20 Human Binding pIC50 = 8.3 8.3 43 2
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 75879 None 20 Human Binding pIC50 = 8.3 8.3 43 2
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 178087 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 178087 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 109321 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 109321 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 109307 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 109307 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 84705 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 84705 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 121573 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
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 121573 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
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 109297 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 109297 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 64613 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 64613 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 110331 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 110331 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 75874 None 0 Human Binding pIC50 = 6.4 6.4 - 1
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 75874 None 0 Human Binding pIC50 = 6.4 6.4 - 1
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 161312 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 161312 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 178221 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 178221 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 137231 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 137231 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 62911 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 62911 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 63460 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 63460 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 121584 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 121584 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 121347 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 121347 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 96949 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 96949 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 496 10 3 6 4.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccco1 10.1021/jm070024h
59446148 175047 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 175047 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 5853 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 5853 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 74419 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 74419 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 163001 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 163001 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 5629 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 5629 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 137206 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 137206 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 109296 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 109296 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 151994 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 151994 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 113461 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 113461 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 98970 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 98970 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 84785 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 84785 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 75871 None 0 Human Binding pIC50 = 6.4 6.4 - 1
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 75871 None 0 Human Binding pIC50 = 6.4 6.4 - 1
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 6349 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 6349 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 155372 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 155372 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 94650 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 94650 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 155416 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 155416 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 141249 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 141249 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 81598 None 0 Human Binding pIC50 = 4.4 4.4 - 0
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 81598 None 0 Human Binding pIC50 = 4.4 4.4 - 0
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 81598 None 0 Human Binding pIC50 = 4.4 4.4 - 0
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 81598 None 0 Human Binding pIC50 = 4.4 4.4 - 0
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 8046 None 0 Human Binding pIC50 = 4.4 4.4 - 0
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 8046 None 0 Human Binding pIC50 = 4.4 4.4 - 0
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 81605 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 81605 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 5821 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 5821 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 98386 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 98386 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 177696 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 177696 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 177648 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 177648 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 174698 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 174698 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 81610 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 81610 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 146081 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 146081 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 169221 None 1 Human Binding pIC50 = 7.3 7.3 - 0
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 169221 None 1 Human Binding pIC50 = 7.3 7.3 - 0
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 121581 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 121581 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 141504 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 141504 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 121585 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
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 121585 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
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 121996 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
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 121996 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
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 84797 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 84797 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 113460 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 113460 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 5739 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 5739 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 12837 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 12837 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 12837 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 209494 None 1 Human Binding pIC50 = 7.3 7.3 - 0
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 169307 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 169307 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 94374 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 94374 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 162713 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 162713 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 151996 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 151996 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 97064 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 97064 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 109306 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 109306 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 177379 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 177379 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 177379 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 177379 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 178087 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 178087 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 109305 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 109305 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 113442 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 113442 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 181038 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 181038 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 76515 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 76515 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 121583 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 121583 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 75972 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 75972 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 122007 None 0 Rat Binding pIC50 = 8.3 8.3 - 0
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 122007 None 0 Rat Binding pIC50 = 8.3 8.3 - 0
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 140883 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 140883 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 94745 None 2 Human Binding pIC50 = 8.3 8.3 - 0
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 94745 None 2 Human Binding pIC50 = 8.3 8.3 - 0
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 94745 None 2 Human Binding pIC50 = 8.3 8.3 - 0
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 94745 None 2 Human Binding pIC50 = 8.3 8.3 - 0
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 122000 None 0 Rat Binding pIC50 = 8.3 8.3 - 0
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 122000 None 0 Rat Binding pIC50 = 8.3 8.3 - 0
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 109311 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 109311 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 76723 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 76723 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 121999 None 0 Rat Binding pIC50 = 8.2 8.2 - 0
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 121999 None 0 Rat Binding pIC50 = 8.2 8.2 - 0
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 76016 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 76016 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 162713 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 162713 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 136550 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 136550 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 109317 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 109317 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 109660 None 0 Human Binding pIC50 = 4.3 4.3 - 0
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 109660 None 0 Human Binding pIC50 = 4.3 4.3 - 0
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 177644 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 177644 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 177648 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 177648 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 162311 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 162311 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 162789 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 162789 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 162804 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 162804 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 177644 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 177644 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 155013 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 155013 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 81596 None 0 Human Binding pIC50 = 4.3 4.3 - 0
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 81596 None 0 Human Binding pIC50 = 4.3 4.3 - 0
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 93264 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 93264 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 109319 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 109319 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 84789 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 84789 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 177875 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 177875 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 162804 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 162804 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 166936 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 166936 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 146936 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 146936 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 215578 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 213961 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 213961 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 98505 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 98505 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 91550 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 91550 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 213927 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 81603 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 81603 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 172972 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 172972 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 213284 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 136281 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 136281 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 166288 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 166288 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 62502 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 62502 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 62943 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 62943 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 121578 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
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 121578 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
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 213947 None 0 Human Binding pIC50 = 4.3 4.3 - 0
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 162311 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 162311 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 84844 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 84844 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 136375 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 136375 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 136375 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 136375 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 146014 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 146014 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 162789 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 162789 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 121583 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
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 121583 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
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 5859 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 5859 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 81597 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 81597 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 81597 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 81597 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 66201 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 66201 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 75565 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 75565 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 166260 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 166260 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 67069 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 67069 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 154978 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 154978 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 214148 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 161749 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 161749 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 109274 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 109274 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 75877 None 0 Human Binding pIC50 = 7.2 7.2 - 1
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 75877 None 0 Human Binding pIC50 = 7.2 7.2 - 1
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 91803 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 91803 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 98505 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 98505 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 11262 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 11262 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 11262 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 62990 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 62990 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 121345 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 121345 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 137025 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 137025 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 137025 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 137025 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 137025 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 137025 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 137025 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 137025 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 153054 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 153054 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 62990 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 62990 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 75063 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 75063 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 165824 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 165824 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 208466 None 38 Human Binding pIC50 = 8.2 8.2 - 1
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 109299 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 109299 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 141007 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 141007 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 116195 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 116195 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 79155 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 79155 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 122006 None 0 Rat Binding pIC50 = 8.2 8.2 - 0
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 122006 None 0 Rat Binding pIC50 = 8.2 8.2 - 0
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 113478 None 1 Human Binding pIC50 = 8.2 8.2 - 0
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 113478 None 1 Human Binding pIC50 = 8.2 8.2 - 0
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 121580 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 121580 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 77351 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 77351 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 154785 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 154785 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 141731 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 141731 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 109315 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 109315 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 213960 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 2232 None 24 Rat Binding pIC50 = 7.2 7.2 - 1
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 2232 None 24 Rat Binding pIC50 = 7.2 7.2 - 1
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 2232 None 24 Rat Binding pIC50 = 7.2 7.2 - 1
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 169552 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 169552 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 98852 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 98852 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 208466 None 38 Human Binding pIC50 = 5.2 5.2 - 1
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 157240 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 157240 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 97038 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 97038 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 76179 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 76179 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 141731 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 141731 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 209056 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 5860 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 5860 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 147017 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 147017 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 2232 None 24 Pig Binding pIC50 = 7.2 7.2 - 1
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 2232 None 24 Pig Binding pIC50 = 7.2 7.2 - 1
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 2232 None 24 Pig Binding pIC50 = 7.2 7.2 - 1
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 177078 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 177078 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 162072 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 162072 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 162940 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 162940 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 76408 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 76408 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 84895 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 84895 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 137189 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 137189 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 121348 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 121348 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 113437 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 113437 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 76425 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 76425 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 115377 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 115377 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 149015 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 149015 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 138136 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 138136 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 78771 None 1 Human Binding pIC50 = 7.2 7.2 - 0
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 78771 None 1 Human Binding pIC50 = 7.2 7.2 - 0
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 144279 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 144279 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 13019 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 13019 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 13019 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 94514 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 94514 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 77332 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 77332 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 177078 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 177078 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 5858 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 5858 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 162940 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 162940 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 5782 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 5782 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 122032 None 12 Human Binding pIC50 = 6.2 6.2 - 0
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 122032 None 12 Human Binding pIC50 = 6.2 6.2 - 0
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 94645 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 94645 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 98663 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 98663 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 74999 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 74999 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 126765 None 0 Mouse Binding pIC50 = 8.2 8.2 - 0
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 126765 None 0 Mouse Binding pIC50 = 8.2 8.2 - 0
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 210573 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 121582 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 121582 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 113481 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 113481 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 109292 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 109292 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 74999 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 74999 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 138534 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 138534 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 109302 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 109302 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 76176 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 76176 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 161721 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 161721 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 79160 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 79160 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 79899 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 79899 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 211767 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 211767 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 94185 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 94185 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 84315 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 84315 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 76739 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 76739 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 162072 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 162072 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 63076 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 63076 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 80214 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 80214 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 121574 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
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 121574 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
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 81619 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 81619 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 81619 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 81619 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 173034 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 173034 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 81611 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 81611 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 67069 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 67069 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 84727 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 84727 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 81607 None 1 Human Binding pIC50 = 6.1 6.1 - 0
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 81607 None 1 Human Binding pIC50 = 6.1 6.1 - 0
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 64581 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 64581 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 91241 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 91241 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 161868 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 161868 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 113458 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 113458 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 64421 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 64421 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 5815 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 5815 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 177628 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 177628 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 211765 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 209322 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 209322 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 137810 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 137810 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 211765 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 177500 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 177500 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 177628 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 177628 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 162993 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 162993 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 161329 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 161329 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 161329 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 177659 None 4 Human Binding pIC50 = 8.1 8.1 - 0
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 177659 None 4 Human Binding pIC50 = 8.1 8.1 - 0
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 94675 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 94675 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 77914 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 77914 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 5808 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 5808 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 12030 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 12030 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 12030 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 125198 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 125198 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 113438 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 113438 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 113435 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 113435 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 113450 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 113450 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 154675 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 154675 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 137500 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 137500 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 559 11 4 5 5.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
122182045 121998 None 0 Rat Binding pIC50 = 7.1 7.1 - 0
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 121998 None 0 Rat Binding pIC50 = 7.1 7.1 - 0
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 94985 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 94985 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 67269 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 67269 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 168351 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 168351 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 81613 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 81613 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 81613 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 81613 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 81600 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 81600 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 81600 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 81600 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 155121 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 155121 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 123237 None 40 Human Binding pIC50 = 5.1 5.1 - 0
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 123237 None 40 Human Binding pIC50 = 5.1 5.1 - 0
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 9285 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 9285 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 12020 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 12020 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 12020 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 168711 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 168711 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 75548 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 75548 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 113463 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 113463 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 122340 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 122340 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 177500 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 177500 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 121573 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 121573 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 121335 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 121335 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 84994 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 84994 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 5707 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 5707 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 136631 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 136631 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 172819 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 172819 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 81609 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 81609 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 81606 None 0 Human Binding pIC50 = 4.1 4.1 - 0
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 81606 None 0 Human Binding pIC50 = 4.1 4.1 - 0
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 75869 None 0 Human Binding pIC50 = 7.1 7.1 - 1
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 75869 None 0 Human Binding pIC50 = 7.1 7.1 - 1
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 75875 None 0 Human Binding pIC50 = 7.1 7.1 - 1
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 75875 None 0 Human Binding pIC50 = 7.1 7.1 - 1
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 168644 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 168644 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 66136 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 66136 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 523 9 1 6 5.7 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL335799 211562 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 215837 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 161897 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 161897 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 162993 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 162993 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 124465 None 1 Human Binding pIC50 = 8.1 8.1 - 0
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 124465 None 1 Human Binding pIC50 = 8.1 8.1 - 0
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 79151 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 79151 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 79151 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 79151 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 123235 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 123235 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 121998 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
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 121998 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
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 75932 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 75932 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 121999 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
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 121999 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
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 91998 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 91998 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 212797 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 74999 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 74999 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 214113 None 0 Human Binding pIC50 = 8.0 8.0 - 1
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 75012 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 75012 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 122000 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
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 122000 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
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 75881 None 0 Human Binding pIC50 = 7.1 7.1 - 1
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 75881 None 0 Human Binding pIC50 = 7.1 7.1 - 1
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 121575 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
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 121575 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
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 123852 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 123852 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 122166 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 122166 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 162264 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 162264 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 97037 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 97037 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 84694 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 84694 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 79161 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 79161 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 77147 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 77147 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 12842 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 12842 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 12842 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 1065 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 1065 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 1065 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 214086 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 5758 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 5758 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 211766 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 211766 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 162513 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 162513 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 109316 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 109316 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 62574 None 1 Human Binding pIC50 = 6.0 6.0 - 0
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 62574 None 1 Human Binding pIC50 = 6.0 6.0 - 0
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 1969 None 33 Human Binding pKd = 9.9 9.9 - 1
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 1969 None 33 Human Binding pKd = 9.9 9.9 - 1
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 1969 None 33 Human Binding pKd = 9.9 9.9 - 1
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 71274 None 0 Human Binding pKi = 11 11.0 - 1
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 71274 None 0 Human Binding pKi = 11 11.0 - 1
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 71275 None 0 Human Binding pKi = 11 11.0 - 1
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 71275 None 0 Human Binding pKi = 11 11.0 - 1
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 71291 None 0 Human Binding pKi = 10.3 10.3 - 1
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 71291 None 0 Human Binding pKi = 10.3 10.3 - 1
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 71282 None 0 Human Binding pKi = 10 10.0 - 1
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 71282 None 0 Human Binding pKi = 10 10.0 - 1
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 69034 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69034 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69035 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69035 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69048 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69048 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69050 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69050 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69051 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69051 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69061 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69061 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69066 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69066 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142824 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142824 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143135 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143135 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143503 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143503 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144048 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144048 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144367 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144367 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144565 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144565 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144612 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144612 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144930 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144930 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145384 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145384 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145445 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145445 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145572 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145572 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145931 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145931 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145935 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145935 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146189 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146189 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146445 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146445 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147375 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147375 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148007 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148007 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148169 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148169 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148685 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148685 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148784 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148784 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150598 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150598 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150630 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150630 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151192 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151192 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151340 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151340 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152283 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152283 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152764 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152764 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154034 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154034 None 0 Human Binding pKi = 10 10.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 71271 None 0 Human Binding pKi = 9.8 9.8 - 1
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 71271 None 0 Human Binding pKi = 9.8 9.8 - 1
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 71272 None 0 Human Binding pKi = 9.7 9.7 - 1
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 71272 None 0 Human Binding pKi = 9.7 9.7 - 1
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 71280 None 0 Human Binding pKi = 9.7 9.7 - 1
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 71280 None 0 Human Binding pKi = 9.7 9.7 - 1
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 1969 None 33 Human Binding pKi = 9.6 9.6 - 1
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 1969 None 33 Human Binding pKi = 9.6 9.6 - 1
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 1969 None 33 Human Binding pKi = 9.6 9.6 - 1
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 71288 None 0 Human Binding pKi = 9.6 9.6 - 1
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 71288 None 0 Human Binding pKi = 9.6 9.6 - 1
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 71290 None 0 Human Binding pKi = 9.6 9.6 - 1
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 71290 None 0 Human Binding pKi = 9.6 9.6 - 1
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 71281 None 0 Human Binding pKi = 9.5 9.5 - 1
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 71281 None 0 Human Binding pKi = 9.5 9.5 - 1
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 69042 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69042 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 113386 None 0 Human Binding pKi = 9.5 9.5 - 1
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 113386 None 0 Human Binding pKi = 9.5 9.5 - 1
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 69042 None 0 Human Binding pKi = 9.5 9.5 - 1
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 69042 None 0 Human Binding pKi = 9.5 9.5 - 1
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 69054 None 0 Human Binding pKi = 9.4 9.4 - 1
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 69054 None 0 Human Binding pKi = 9.4 9.4 - 1
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 71278 None 0 Human Binding pKi = 9.4 9.4 - 1
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 71278 None 0 Human Binding pKi = 9.4 9.4 - 1
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 181223 None 0 Human Binding pKi = 9.4 9.4 - 1
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 181223 None 0 Human Binding pKi = 9.4 9.4 - 1
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 110519 None 0 Human Binding pKi = 9.4 9.4 - 1
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 110519 None 0 Human Binding pKi = 9.4 9.4 - 1
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 71284 None 0 Human Binding pKi = 9.3 9.3 - 1
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 71284 None 0 Human Binding pKi = 9.3 9.3 - 1
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 181115 None 0 Human Binding pKi = 9.3 9.3 - 1
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 181115 None 0 Human Binding pKi = 9.3 9.3 - 1
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 71286 None 0 Human Binding pKi = 9.2 9.2 - 1
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 71286 None 0 Human Binding pKi = 9.2 9.2 - 1
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 183020 None 0 Human Binding pKi = 9.2 9.2 - 1
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 183020 None 0 Human Binding pKi = 9.2 9.2 - 1
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 214113 None 0 Human Binding pKi = 9.2 9.2 - 1
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 125193 None 0 Human Binding pKi = 9.1 9.1 - 1
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 125193 None 0 Human Binding pKi = 9.1 9.1 - 1
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 69064 None 0 Human Binding pKi = 9.1 9.1 - 1
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 69064 None 0 Human Binding pKi = 9.1 9.1 - 1
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 71273 None 0 Human Binding pKi = 9.1 9.1 - 1
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 71273 None 0 Human Binding pKi = 9.1 9.1 - 1
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 179724 None 0 Human Binding pKi = 9 9.0 - 1
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 179724 None 0 Human Binding pKi = 9 9.0 - 1
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 172955 None 0 Human Binding pKi = 8.9 8.9 - 1
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 172955 None 0 Human Binding pKi = 8.9 8.9 - 1
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 213329 None 18 Human Binding pKi = 8.9 8.9 - 1
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 213329 None 18 Human Binding pKi = 8.9 8.9 - 1
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 180480 None 0 Human Binding pKi = 8.9 8.9 - 1
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 180480 None 0 Human Binding pKi = 8.9 8.9 - 1
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 71287 None 0 Human Binding pKi = 8.8 8.8 - 1
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 71287 None 0 Human Binding pKi = 8.8 8.8 - 1
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 71267 None 0 Human Binding pKi = 8.8 8.8 - 1
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 71267 None 0 Human Binding pKi = 8.8 8.8 - 1
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 71289 None 0 Human Binding pKi = 8.7 8.7 - 1
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 71289 None 0 Human Binding pKi = 8.7 8.7 - 1
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 69011 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69011 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69033 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69033 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69041 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69041 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69049 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69049 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69059 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69059 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69060 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69060 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69062 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69062 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69067 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69067 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142371 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142371 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142394 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142394 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142466 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142466 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142505 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142505 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142541 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142541 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142600 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142600 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142874 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142874 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142897 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142897 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143234 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143234 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143349 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143349 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143350 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143350 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143451 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143451 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143692 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143692 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144009 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144009 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144659 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144659 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144811 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144811 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144861 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144861 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144862 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144862 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145158 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145158 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145182 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145182 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145285 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145285 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145324 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145324 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145373 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145373 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145758 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145758 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145856 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145856 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146060 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146060 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146371 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146371 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146402 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146402 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146552 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146552 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146651 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146651 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146727 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146727 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146788 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146788 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146992 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146992 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147116 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147116 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147411 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147411 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147750 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147750 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147753 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147753 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148012 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148012 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148352 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148352 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148451 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148451 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148472 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148472 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148518 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148518 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148541 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148541 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148778 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148778 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149017 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149017 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149088 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149088 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149102 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149102 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149124 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149124 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149447 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149447 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149487 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149487 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149761 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149761 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149783 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149783 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150089 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150089 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150148 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150148 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150272 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150272 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150284 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150284 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150329 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150329 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150333 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150333 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151010 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151010 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151012 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151012 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151090 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151090 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151377 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151377 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151644 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151644 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152113 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152113 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152154 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152154 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152297 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152297 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152440 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152440 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152530 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152530 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152718 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152718 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152897 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152897 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153059 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153059 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153102 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153102 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153166 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153166 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153317 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153317 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153457 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153457 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153521 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153521 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153670 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153670 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153856 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153856 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153955 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153955 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154052 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154052 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154260 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154260 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154298 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154298 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 125191 None 0 Human Binding pKi = 8 8.0 - 1
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 125191 None 0 Human Binding pKi = 8 8.0 - 1
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 179734 None 0 Human Binding pKi = 8 8.0 - 1
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 179734 None 0 Human Binding pKi = 8 8.0 - 1
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 182133 None 0 Human Binding pKi = 8 8.0 - 1
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 182133 None 0 Human Binding pKi = 8 8.0 - 1
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 92283 None 0 Human Binding pKi = 8.0 8.0 2089 2
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 92283 None 0 Human Binding pKi = 8.0 8.0 2089 2
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 111733 None 0 Human Binding pKi = 8.0 8.0 - 1
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 111733 None 0 Human Binding pKi = 8.0 8.0 - 1
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 69013 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69013 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69015 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69015 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69016 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69016 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69017 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69017 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69038 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69038 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69055 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69055 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69057 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69057 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69058 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69058 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 83527 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 83527 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142393 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142393 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142633 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142633 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142718 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142718 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142752 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142752 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142917 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142917 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143339 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143339 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143517 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143517 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143666 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143666 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143675 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143675 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143729 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143729 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143992 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143992 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144077 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144077 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144113 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144113 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144136 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144136 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144330 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144330 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144390 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144390 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144483 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144483 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144509 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144509 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144563 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144563 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144647 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144647 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144699 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144699 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144926 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144926 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144969 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144969 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145136 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145136 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145208 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145208 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145341 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145341 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145400 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145400 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145458 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145458 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145471 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145471 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145734 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145734 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145932 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145932 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146337 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146337 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146618 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146618 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146663 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146663 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146693 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146693 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147223 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147223 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147385 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147385 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147552 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147552 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147634 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147634 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147663 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147663 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147972 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147972 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147984 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147984 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148074 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148074 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148132 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148132 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148163 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148163 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148316 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148316 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148363 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148363 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148477 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148477 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148603 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148603 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148697 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148697 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148800 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148800 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149021 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149021 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149024 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149024 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149028 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149028 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149032 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149032 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149113 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149113 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149311 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149311 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149433 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149433 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149444 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149444 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149696 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149696 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149815 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149815 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149855 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149855 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149936 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149936 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149964 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149964 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150110 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150110 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150139 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150139 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150155 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150155 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150450 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150450 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150487 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150487 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150525 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150525 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150655 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150655 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151035 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151035 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151048 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151048 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151349 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151349 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151400 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151400 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151408 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151408 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151546 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151546 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151603 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151603 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151821 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151821 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151824 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151824 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151854 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151854 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151923 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151923 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152077 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152077 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152368 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152368 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152392 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152392 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152400 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152400 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152401 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152401 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152446 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152446 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152509 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152509 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152577 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152577 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152742 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152742 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152823 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152823 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153206 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153206 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153210 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153210 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153216 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153216 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153352 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153352 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153378 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153378 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153400 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153400 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153481 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153481 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153564 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153564 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153629 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153629 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153649 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153649 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153746 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153746 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153759 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153759 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154150 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154150 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154344 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154344 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69012 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69012 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69014 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69014 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143632 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143632 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143682 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143682 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143931 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143931 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143962 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143962 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146207 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146207 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146244 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146244 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146275 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146275 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146368 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146368 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146637 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146637 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146642 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146642 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146726 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146726 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147481 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147481 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148279 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148279 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148482 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148482 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148634 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148634 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149592 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149592 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149934 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149934 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151016 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151016 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151086 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151086 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151125 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151125 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151348 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151348 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151562 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151562 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151832 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151832 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152045 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152045 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152078 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152078 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152865 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152865 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152870 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152870 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152914 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152914 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153174 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153174 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153198 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153198 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153553 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153553 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153668 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153668 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153697 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153697 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154092 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154092 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154204 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154204 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69044 None 0 Human Binding pKi = 7.0 7.0 - 1
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 69044 None 0 Human Binding pKi = 7.0 7.0 - 1
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 148028 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148028 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147862 None 0 Human Binding pKi = 6.0 6.0 - 1
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 147862 None 0 Human Binding pKi = 6.0 6.0 - 1
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 75873 None 0 Human Binding pKi = 8.0 8.0 - 1
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 75873 None 0 Human Binding pKi = 8.0 8.0 - 1
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 139705 None 0 Human Binding pKi = 8.0 8.0 - 1
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 139705 None 0 Human Binding pKi = 8.0 8.0 - 1
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 139692 None 0 Human Binding pKi = 7.0 7.0 - 1
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 139692 None 0 Human Binding pKi = 7.0 7.0 - 1
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 69014 None 0 Human Binding pKi = 6.0 6.0 - 1
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 69014 None 0 Human Binding pKi = 6.0 6.0 - 1
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 92263 None 0 Human Binding pKi = 6.0 6.0 1 2
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 92263 None 0 Human Binding pKi = 6.0 6.0 1 2
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 75874 None 0 Human Binding pKi = 6.9 6.9 - 1
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 75874 None 0 Human Binding pKi = 6.9 6.9 - 1
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 182233 None 0 Human Binding pKi = 6.9 6.9 - 1
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 182233 None 0 Human Binding pKi = 6.9 6.9 - 1
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 67529 None 0 Human Binding pKi = 5.9 5.9 - 1
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 67529 None 0 Human Binding pKi = 5.9 5.9 - 1
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 66941 None 0 Human Binding pKi = 5.9 5.9 - 1
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 66941 None 0 Human Binding pKi = 5.9 5.9 - 1
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 67354 None 0 Human Binding pKi = 5.9 5.9 - 1
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 67354 None 0 Human Binding pKi = 5.9 5.9 - 1
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 69063 None 0 Human Binding pKi = 7.9 7.9 - 1
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 69063 None 0 Human Binding pKi = 7.9 7.9 - 1
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 125195 None 0 Human Binding pKi = 7.9 7.9 - 1
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 125195 None 0 Human Binding pKi = 7.9 7.9 - 1
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 179876 None 0 Human Binding pKi = 7.9 7.9 - 1
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 179876 None 0 Human Binding pKi = 7.9 7.9 - 1
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 111736 None 0 Human Binding pKi = 7.9 7.9 - 1
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 111736 None 0 Human Binding pKi = 7.9 7.9 - 1
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 69017 None 0 Human Binding pKi = 6.9 6.9 - 1
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 69017 None 0 Human Binding pKi = 6.9 6.9 - 1
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 69012 None 0 Human Binding pKi = 5.9 5.9 - 1
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 69012 None 0 Human Binding pKi = 5.9 5.9 - 1
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 81841 None 0 Human Binding pKi = 6.9 6.9 - 1
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 81841 None 0 Human Binding pKi = 6.9 6.9 - 1
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 182150 None 0 Human Binding pKi = 6.9 6.9 - 1
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 182150 None 0 Human Binding pKi = 6.9 6.9 - 1
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 117192 None 0 Human Binding pKi = 6.9 6.9 - 1
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 117192 None 0 Human Binding pKi = 6.9 6.9 - 1
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 168858 None 0 Human Binding pKi = 5.9 5.9 - 1
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 168858 None 0 Human Binding pKi = 5.9 5.9 - 1
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 66766 None 4 Human Binding pKi = 5.9 5.9 - 1
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 66766 None 4 Human Binding pKi = 5.9 5.9 - 1
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 69037 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69037 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 117188 None 0 Human Binding pKi = 7.9 7.9 - 1
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 117188 None 0 Human Binding pKi = 7.9 7.9 - 1
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 180981 None 0 Human Binding pKi = 7.9 7.9 - 1
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 180981 None 0 Human Binding pKi = 7.9 7.9 - 1
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 181146 None 0 Human Binding pKi = 6.9 6.9 - 1
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 181146 None 0 Human Binding pKi = 6.9 6.9 - 1
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 181408 None 0 Human Binding pKi = 6.9 6.9 - 1
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 181408 None 0 Human Binding pKi = 6.9 6.9 - 1
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 139717 None 0 Human Binding pKi = 6.9 6.9 - 1
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 139717 None 0 Human Binding pKi = 6.9 6.9 - 1
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 124268 None 4 Human Binding pKi = 5.9 5.9 - 1
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 124268 None 4 Human Binding pKi = 5.9 5.9 - 1
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 180194 None 0 Human Binding pKi = 6.9 6.9 - 1
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 180194 None 0 Human Binding pKi = 6.9 6.9 - 1
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 67351 None 5 Human Binding pKi = 5.9 5.9 - 1
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 67351 None 5 Human Binding pKi = 5.9 5.9 - 1
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 90191 None 0 Human Binding pKi = 5.9 5.9 - 1
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 90191 None 0 Human Binding pKi = 5.9 5.9 - 1
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 92276 None 0 Human Binding pKi = 5.9 5.9 1 2
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 92276 None 0 Human Binding pKi = 5.9 5.9 1 2
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 117193 None 0 Human Binding pKi = 6.9 6.9 - 1
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 117193 None 0 Human Binding pKi = 6.9 6.9 - 1
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 75872 None 0 Human Binding pKi = 7.9 7.9 - 1
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 75872 None 0 Human Binding pKi = 7.9 7.9 - 1
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 75876 None 0 Human Binding pKi = 7.9 7.9 - 1
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 75876 None 0 Human Binding pKi = 7.9 7.9 - 1
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 75881 None 0 Human Binding pKi = 7.9 7.9 - 1
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 75881 None 0 Human Binding pKi = 7.9 7.9 - 1
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 111736 None 0 Human Binding pKi = 7.9 7.9 - 1
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 111736 None 0 Human Binding pKi = 7.9 7.9 - 1
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 181217 None 0 Human Binding pKi = 7.9 7.9 - 1
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 181217 None 0 Human Binding pKi = 7.9 7.9 - 1
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 182829 None 0 Human Binding pKi = 7.9 7.9 - 1
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 182829 None 0 Human Binding pKi = 7.9 7.9 - 1
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 116194 None 0 Human Binding pKi = 7.8 7.8 - 1
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 116194 None 0 Human Binding pKi = 7.8 7.8 - 1
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 69046 None 0 Human Binding pKi = 7.8 7.8 - 1
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 69046 None 0 Human Binding pKi = 7.8 7.8 - 1
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 92282 None 0 Human Binding pKi = 7.8 7.8 1819 2
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 92282 None 0 Human Binding pKi = 7.8 7.8 1819 2
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 111735 None 0 Human Binding pKi = 7.8 7.8 - 1
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 111735 None 0 Human Binding pKi = 7.8 7.8 - 1
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 69055 None 0 Human Binding pKi = 5.8 5.8 - 1
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 69055 None 0 Human Binding pKi = 5.8 5.8 - 1
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 75871 None 0 Human Binding pKi = 6.8 6.8 - 1
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 75871 None 0 Human Binding pKi = 6.8 6.8 - 1
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 139931 None 0 Human Binding pKi = 6.8 6.8 - 1
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 139931 None 0 Human Binding pKi = 6.8 6.8 - 1
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 139970 None 0 Human Binding pKi = 6.8 6.8 - 1
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 139970 None 0 Human Binding pKi = 6.8 6.8 - 1
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 89775 None 0 Human Binding pKi = 5.8 5.8 - 1
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 89775 None 0 Human Binding pKi = 5.8 5.8 - 1
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 69036 None 0 Human Binding pKi = 7.8 7.8 - 1
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 69036 None 0 Human Binding pKi = 7.8 7.8 - 1
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 71600 None 17 Human Binding pKi = 7.8 7.8 - 1
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 71600 None 17 Human Binding pKi = 7.8 7.8 - 1
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 71600 None 17 Human Binding pKi = 7.8 7.8 - 1
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 92260 None 0 Human Binding pKi = 7.8 7.8 - 1
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 92260 None 0 Human Binding pKi = 7.8 7.8 - 1
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 111736 None 0 Human Binding pKi = 7.8 7.8 - 1
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 111736 None 0 Human Binding pKi = 7.8 7.8 - 1
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 69056 None 0 Human Binding pKi = 6.8 6.8 - 1
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 69056 None 0 Human Binding pKi = 6.8 6.8 - 1
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 181081 None 0 Human Binding pKi = 5.8 5.8 - 1
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 181081 None 0 Human Binding pKi = 5.8 5.8 - 1
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 117187 None 0 Human Binding pKi = 6.8 6.8 - 1
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 117187 None 0 Human Binding pKi = 6.8 6.8 - 1
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 181314 None 0 Human Binding pKi = 6.8 6.8 - 1
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 181314 None 0 Human Binding pKi = 6.8 6.8 - 1
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 92265 None 0 Human Binding pKi = 5.8 5.8 1 2
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 92265 None 0 Human Binding pKi = 5.8 5.8 1 2
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 75877 None 0 Human Binding pKi = 7.8 7.8 - 1
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 75877 None 0 Human Binding pKi = 7.8 7.8 - 1
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 139859 None 0 Human Binding pKi = 7.8 7.8 - 1
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 139859 None 0 Human Binding pKi = 7.8 7.8 - 1
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 139941 None 0 Human Binding pKi = 7.8 7.8 - 1
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 139941 None 0 Human Binding pKi = 7.8 7.8 - 1
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 183507 None 0 Human Binding pKi = 7.8 7.8 - 1
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 183507 None 0 Human Binding pKi = 7.8 7.8 - 1
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 92271 None 0 Human Binding pKi = 7.8 7.8 1548 2
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 92271 None 0 Human Binding pKi = 7.8 7.8 1548 2
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 146279 None 0 Human Binding pKi = 5.8 5.8 - 1
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 146279 None 0 Human Binding pKi = 5.8 5.8 - 1
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 147681 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147681 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 88771 None 0 Human Binding pKi = 5.8 5.8 - 1
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 88771 None 0 Human Binding pKi = 5.8 5.8 - 1
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 139612 None 0 Human Binding pKi = 7.8 7.8 - 1
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 139612 None 0 Human Binding pKi = 7.8 7.8 - 1
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 9312 None 0 Human Binding pKi = 7.8 7.8 - 1
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 9312 None 0 Human Binding pKi = 7.8 7.8 - 1
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 69065 None 0 Human Binding pKi = 7.7 7.7 - 1
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 69065 None 0 Human Binding pKi = 7.7 7.7 - 1
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 90029 None 0 Human Binding pKi = 6.7 6.7 - 1
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 90029 None 0 Human Binding pKi = 6.7 6.7 - 1
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 145448 None 0 Human Binding pKi = 5.7 5.7 - 1
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 145448 None 0 Human Binding pKi = 5.7 5.7 - 1
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 67275 None 0 Human Binding pKi = 5.7 5.7 - 1
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 67275 None 0 Human Binding pKi = 5.7 5.7 - 1
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 167495 None 0 Human Binding pKi = 8.7 8.7 - 1
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 167495 None 0 Human Binding pKi = 8.7 8.7 - 1
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 71268 None 0 Human Binding pKi = 8.7 8.7 - 1
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 71268 None 0 Human Binding pKi = 8.7 8.7 - 1
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 125194 None 0 Human Binding pKi = 8.7 8.7 - 1
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 125194 None 0 Human Binding pKi = 8.7 8.7 - 1
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 179836 None 0 Human Binding pKi = 8.6 8.6 - 1
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 179836 None 0 Human Binding pKi = 8.6 8.6 - 1
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 139564 None 0 Human Binding pKi = 8.6 8.6 - 1
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 139564 None 0 Human Binding pKi = 8.6 8.6 - 1
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 69066 None 0 Human Binding pKi = 8.6 8.6 - 1
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 69066 None 0 Human Binding pKi = 8.6 8.6 - 1
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 71277 None 0 Human Binding pKi = 8.6 8.6 - 1
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 71277 None 0 Human Binding pKi = 8.6 8.6 - 1
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 171438 None 0 Human Binding pKi = 8.6 8.6 - 1
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 171438 None 0 Human Binding pKi = 8.6 8.6 - 1
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 75869 None 0 Human Binding pKi = 7.7 7.7 - 1
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 75869 None 0 Human Binding pKi = 7.7 7.7 - 1
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 117194 None 0 Human Binding pKi = 7.7 7.7 - 1
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 117194 None 0 Human Binding pKi = 7.7 7.7 - 1
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 89909 None 0 Human Binding pKi = 6.7 6.7 - 1
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 89909 None 0 Human Binding pKi = 6.7 6.7 - 1
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 179869 None 0 Human Binding pKi = 6.7 6.7 - 1
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 179869 None 0 Human Binding pKi = 6.7 6.7 - 1
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 81899 None 0 Human Binding pKi = 6.7 6.7 - 1
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 81899 None 0 Human Binding pKi = 6.7 6.7 - 1
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 66771 None 5 Human Binding pKi = 5.7 5.7 - 1
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 66771 None 5 Human Binding pKi = 5.7 5.7 - 1
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 75880 None 0 Human Binding pKi = 6.7 6.7 - 1
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 75880 None 0 Human Binding pKi = 6.7 6.7 - 1
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 69049 None 0 Human Binding pKi = 7.7 7.7 - 1
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 69049 None 0 Human Binding pKi = 7.7 7.7 - 1
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 139629 None 0 Human Binding pKi = 6.7 6.7 - 1
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 139629 None 0 Human Binding pKi = 6.7 6.7 - 1
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 69058 None 0 Human Binding pKi = 6.7 6.7 - 1
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 69058 None 0 Human Binding pKi = 6.7 6.7 - 1
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 75865 None 0 Human Binding pKi = 6.7 6.7 - 1
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 75865 None 0 Human Binding pKi = 6.7 6.7 - 1
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 167451 None 0 Human Binding pKi = 5.7 5.7 - 1
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 167451 None 0 Human Binding pKi = 5.7 5.7 - 1
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 61179 None 0 Human Binding pKi = 7.7 7.7 - 1
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 61179 None 0 Human Binding pKi = 7.7 7.7 - 1
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 209359 None 0 Human Binding pKi = 7.7 7.7 - 1
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 123791 None 0 Human Binding pKi = 6.7 6.7 - 1
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 123791 None 0 Human Binding pKi = 6.7 6.7 - 1
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 139734 None 0 Human Binding pKi = 6.7 6.7 - 1
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 139734 None 0 Human Binding pKi = 6.7 6.7 - 1
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 181968 None 0 Human Binding pKi = 6.7 6.7 - 1
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 181968 None 0 Human Binding pKi = 6.7 6.7 - 1
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 186901 None 0 Human Binding pKi = 5.7 5.7 - 1
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 186901 None 0 Human Binding pKi = 5.7 5.7 - 1
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 89598 None 0 Human Binding pKi = 5.7 5.7 - 1
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 89598 None 0 Human Binding pKi = 5.7 5.7 - 1
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 75882 None 0 Human Binding pKi = 7.6 7.6 - 1
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 75882 None 0 Human Binding pKi = 7.6 7.6 - 1
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 181389 None 0 Human Binding pKi = 7.6 7.6 - 1
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 181389 None 0 Human Binding pKi = 7.6 7.6 - 1
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 180374 None 0 Human Binding pKi = 6.6 6.6 - 1
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 180374 None 0 Human Binding pKi = 6.6 6.6 - 1
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 209364 None 0 Human Binding pKi = 6.6 6.6 - 1
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 146532 None 0 Human Binding pKi = 5.6 5.6 - 1
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 146532 None 0 Human Binding pKi = 5.6 5.6 - 1
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 88510 None 0 Human Binding pKi = 5.6 5.6 - 1
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 88510 None 0 Human Binding pKi = 5.6 5.6 - 1
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 188050 None 0 Human Binding pKi = 6.6 6.6 -69 8
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 188050 None 0 Human Binding pKi = 6.6 6.6 -69 8
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 209365 None 0 Human Binding pKi = 6.6 6.6 - 1
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 81901 None 0 Human Binding pKi = 6.6 6.6 - 1
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 81901 None 0 Human Binding pKi = 6.6 6.6 - 1
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 75875 None 0 Human Binding pKi = 7.6 7.6 - 1
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 75875 None 0 Human Binding pKi = 7.6 7.6 - 1
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 69033 None 0 Human Binding pKi = 7.6 7.6 - 1
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 69033 None 0 Human Binding pKi = 7.6 7.6 - 1
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 92274 None 0 Human Binding pKi = 7.6 7.6 524 2
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 92274 None 0 Human Binding pKi = 7.6 7.6 524 2
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 187046 None 0 Human Binding pKi = 6.6 6.6 - 1
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 187046 None 0 Human Binding pKi = 6.6 6.6 - 1
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 92264 None 0 Human Binding pKi = 4.6 4.6 -1 2
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 92264 None 0 Human Binding pKi = 4.6 4.6 -1 2
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 214220 None 0 Human Binding pKi = 6.6 6.6 - 1
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 214220 None 0 Human Binding pKi = 6.6 6.6 - 1
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 214220 None 0 Human Binding pKi = 6.6 6.6 - 1
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 214220 None 0 Human Binding pKi = 6.6 6.6 - 1
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 186833 None 0 Human Binding pKi = 6.6 6.6 - 1
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 186833 None 0 Human Binding pKi = 6.6 6.6 - 1
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 117191 None 0 Human Binding pKi = 6.6 6.6 - 1
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 117191 None 0 Human Binding pKi = 6.6 6.6 - 1
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 67406 None 0 Human Binding pKi = 5.6 5.6 - 1
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 67406 None 0 Human Binding pKi = 5.6 5.6 - 1
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 154671 None 0 Human Binding pKi = 5.6 5.6 - 1
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 154671 None 0 Human Binding pKi = 5.6 5.6 - 1
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 75883 None 0 Human Binding pKi = 7.6 7.6 - 1
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 75883 None 0 Human Binding pKi = 7.6 7.6 - 1
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 92261 None 0 Human Binding pKi = 7.6 7.6 - 1
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 92261 None 0 Human Binding pKi = 7.6 7.6 - 1
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 92270 None 0 Human Binding pKi = 6.6 6.6 4 2
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 92270 None 0 Human Binding pKi = 6.6 6.6 4 2
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 117195 None 0 Human Binding pKi = 7.6 7.6 - 1
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 117195 None 0 Human Binding pKi = 7.6 7.6 - 1
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 183356 None 0 Human Binding pKi = 7.6 7.6 - 1
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 183356 None 0 Human Binding pKi = 7.6 7.6 - 1
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 126829 None 3 Human Binding pKi = 6.6 6.6 - 1
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 126829 None 3 Human Binding pKi = 6.6 6.6 - 1
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 81849 None 0 Human Binding pKi = 6.5 6.5 - 1
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 81849 None 0 Human Binding pKi = 6.5 6.5 - 1
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 92274 None 0 Human Binding pKi = 7.5 7.5 524 2
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 92274 None 0 Human Binding pKi = 7.5 7.5 524 2
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 92274 None 0 Human Binding pKi = 7.5 7.5 524 2
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 92274 None 0 Human Binding pKi = 7.5 7.5 524 2
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 88704 None 0 Human Binding pKi = 5.5 5.5 - 1
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 88704 None 0 Human Binding pKi = 5.5 5.5 - 1
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 139692 None 0 Human Binding pKi = 8.5 8.5 - 1
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 139692 None 0 Human Binding pKi = 8.5 8.5 - 1
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 139697 None 0 Human Binding pKi = 8.5 8.5 - 1
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 139697 None 0 Human Binding pKi = 8.5 8.5 - 1
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 139697 None 0 Human Binding pKi = 8.5 8.5 - 1
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 139697 None 0 Human Binding pKi = 8.5 8.5 - 1
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 140061 None 0 Human Binding pKi = 8.5 8.5 - 1
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 140061 None 0 Human Binding pKi = 8.5 8.5 - 1
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 81848 None 0 Human Binding pKi = 8.5 8.5 - 1
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 81848 None 0 Human Binding pKi = 8.5 8.5 - 1
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 180543 None 0 Human Binding pKi = 8.5 8.5 - 1
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 180543 None 0 Human Binding pKi = 8.5 8.5 - 1
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 181778 None 0 Human Binding pKi = 8.5 8.5 - 1
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 181778 None 0 Human Binding pKi = 8.5 8.5 - 1
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 172314 None 0 Human Binding pKi = 8.5 8.5 - 1
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 172314 None 0 Human Binding pKi = 8.5 8.5 - 1
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 71276 None 0 Human Binding pKi = 8.5 8.5 - 1
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 71276 None 0 Human Binding pKi = 8.5 8.5 - 1
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 71285 None 0 Human Binding pKi = 8.5 8.5 - 1
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 71285 None 0 Human Binding pKi = 8.5 8.5 - 1
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 92280 None 0 Human Binding pKi = 8.5 8.5 - 1
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 92280 None 0 Human Binding pKi = 8.5 8.5 - 1
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 71279 None 0 Human Binding pKi = 8.5 8.5 - 1
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 71279 None 0 Human Binding pKi = 8.5 8.5 - 1
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 171034 None 0 Human Binding pKi = 8.5 8.5 - 1
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 171034 None 0 Human Binding pKi = 8.5 8.5 - 1
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 182047 None 0 Human Binding pKi = 8.5 8.5 - 1
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 182047 None 0 Human Binding pKi = 8.5 8.5 - 1
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 174585 None 0 Human Binding pKi = 8.4 8.4 - 1
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 174585 None 0 Human Binding pKi = 8.4 8.4 - 1
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 209366 None 15 Human Binding pKi = 8.4 8.4 - 1
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 209366 None 15 Human Binding pKi = 8.4 8.4 - 1
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 92277 None 0 Human Binding pKi = 8.4 8.4 - 1
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 92277 None 0 Human Binding pKi = 8.4 8.4 - 1
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 186900 None 0 Human Binding pKi = 7.5 7.5 - 1
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 186900 None 0 Human Binding pKi = 7.5 7.5 - 1
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 191456 None 0 Human Binding pKi = 7.5 7.5 - 1
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 191456 None 0 Human Binding pKi = 7.5 7.5 - 1
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 139765 None 0 Human Binding pKi = 7.5 7.5 - 1
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 139765 None 0 Human Binding pKi = 7.5 7.5 - 1
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 180471 None 0 Human Binding pKi = 7.5 7.5 - 1
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 180471 None 0 Human Binding pKi = 7.5 7.5 - 1
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 186821 None 0 Human Binding pKi = 6.5 6.5 - 1
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 186821 None 0 Human Binding pKi = 6.5 6.5 - 1
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 182508 None 0 Human Binding pKi = 6.5 6.5 - 1
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 182508 None 0 Human Binding pKi = 6.5 6.5 - 1
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 209351 None 0 Human Binding pKi = 7.5 7.5 - 1
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 89906 None 0 Human Binding pKi = 5.5 5.5 - 1
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 89906 None 0 Human Binding pKi = 5.5 5.5 - 1
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 69045 None 0 Human Binding pKi = 7.5 7.5 - 1
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 69045 None 0 Human Binding pKi = 7.5 7.5 - 1
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 89905 None 0 Human Binding pKi = 6.5 6.5 - 1
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 89905 None 0 Human Binding pKi = 6.5 6.5 - 1
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 88573 None 0 Human Binding pKi = 5.5 5.5 - 1
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 88573 None 0 Human Binding pKi = 5.5 5.5 - 1
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 69043 None 0 Human Binding pKi = 7.5 7.5 - 1
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 69043 None 0 Human Binding pKi = 7.5 7.5 - 1
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 69047 None 0 Human Binding pKi = 7.5 7.5 - 1
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 69047 None 0 Human Binding pKi = 7.5 7.5 - 1
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 209352 None 0 Human Binding pKi = 7.5 7.5 - 1
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 69039 None 0 Human Binding pKi = 7.5 7.5 - 1
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 69039 None 0 Human Binding pKi = 7.5 7.5 - 1
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 180529 None 0 Human Binding pKi = 7.5 7.5 - 1
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 180529 None 0 Human Binding pKi = 7.5 7.5 - 1
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 92262 None 0 Human Binding pKi = 5.4 5.4 1 2
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 92262 None 0 Human Binding pKi = 5.4 5.4 1 2
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 183385 None 0 Human Binding pKi = 6.4 6.4 - 1
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 183385 None 0 Human Binding pKi = 6.4 6.4 - 1
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 69013 None 0 Human Binding pKi = 6.4 6.4 - 1
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 69013 None 0 Human Binding pKi = 6.4 6.4 - 1
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 69040 None 0 Human Binding pKi = 6.4 6.4 - 1
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 69040 None 0 Human Binding pKi = 6.4 6.4 - 1
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 81836 None 0 Human Binding pKi = 6.4 6.4 - 1
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 81836 None 0 Human Binding pKi = 6.4 6.4 - 1
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 4110 None 23 Human Binding pKi = 8.4 8.4 - 1
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 4110 None 23 Human Binding pKi = 8.4 8.4 - 1
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 4110 None 23 Human Binding pKi = 8.4 8.4 - 1
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 139955 None 0 Human Binding pKi = 8.4 8.4 - 1
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 139955 None 0 Human Binding pKi = 8.4 8.4 - 1
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 117189 None 0 Human Binding pKi = 8.4 8.4 - 1
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 117189 None 0 Human Binding pKi = 8.4 8.4 - 1
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 182028 None 0 Human Binding pKi = 8.4 8.4 - 1
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 182028 None 0 Human Binding pKi = 8.4 8.4 - 1
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 69035 None 0 Human Binding pKi = 8.4 8.4 - 1
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 69035 None 0 Human Binding pKi = 8.4 8.4 - 1
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 73189 None 0 Human Binding pKi = 8.4 8.4 - 1
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 73189 None 0 Human Binding pKi = 8.4 8.4 - 1
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 111732 None 0 Human Binding pKi = 8.3 8.3 - 1
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 111732 None 0 Human Binding pKi = 8.3 8.3 - 1
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 69053 None 0 Human Binding pKi = 8.3 8.3 - 1
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 69053 None 0 Human Binding pKi = 8.3 8.3 - 1
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 209366 None 15 Human Binding pKi = 8.3 8.3 - 1
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 209366 None 15 Human Binding pKi = 8.3 8.3 - 1
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 69016 None 0 Human Binding pKi = 6.4 6.4 - 1
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 69016 None 0 Human Binding pKi = 6.4 6.4 - 1
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 69057 None 0 Human Binding pKi = 6.4 6.4 - 1
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 69057 None 0 Human Binding pKi = 6.4 6.4 - 1
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 75865 None 0 Human Binding pKi = 6.4 6.4 - 1
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 75865 None 0 Human Binding pKi = 6.4 6.4 - 1
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 75865 None 0 Human Binding pKi = 6.4 6.4 - 1
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 75865 None 0 Human Binding pKi = 6.4 6.4 - 1
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 145548 None 0 Human Binding pKi = 5.4 5.4 - 1
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 145548 None 0 Human Binding pKi = 5.4 5.4 - 1
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 69041 None 0 Human Binding pKi = 7.4 7.4 - 1
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 69041 None 0 Human Binding pKi = 7.4 7.4 - 1
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 154895 None 24 Human Binding pKi = 7.4 7.4 - 1
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 154895 None 24 Human Binding pKi = 7.4 7.4 - 1
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 81907 None 0 Human Binding pKi = 7.4 7.4 - 1
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 81907 None 0 Human Binding pKi = 7.4 7.4 - 1
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 199930 None 44 Human Binding pKi = 5.4 5.4 -457 5
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 199930 None 44 Human Binding pKi = 5.4 5.4 -457 5
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 75867 None 0 Human Binding pKi = 6.4 6.4 - 1
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 75867 None 0 Human Binding pKi = 6.4 6.4 - 1
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 89303 None 0 Human Binding pKi = 5.4 5.4 - 1
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 89303 None 0 Human Binding pKi = 5.4 5.4 - 1
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 125196 None 0 Human Binding pKi = 7.3 7.3 - 1
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 125196 None 0 Human Binding pKi = 7.3 7.3 - 1
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 139759 None 0 Human Binding pKi = 7.3 7.3 - 1
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 139759 None 0 Human Binding pKi = 7.3 7.3 - 1
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 97011 None 0 Human Binding pKi = 6.3 6.3 -134 6
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 97011 None 0 Human Binding pKi = 6.3 6.3 -134 6
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 88647 None 0 Human Binding pKi = 6.3 6.3 - 1
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 88647 None 0 Human Binding pKi = 6.3 6.3 - 1
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 89413 None 0 Human Binding pKi = 5.3 5.3 - 1
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 89413 None 0 Human Binding pKi = 5.3 5.3 - 1
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 117185 None 0 Human Binding pKi = 7.3 7.3 - 1
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 117185 None 0 Human Binding pKi = 7.3 7.3 - 1
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 69052 None 0 Human Binding pKi = 8.3 8.3 - 1
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 69052 None 0 Human Binding pKi = 8.3 8.3 - 1
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 71292 None 0 Human Binding pKi = 8.3 8.3 - 1
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 71292 None 0 Human Binding pKi = 8.3 8.3 - 1
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 9138 None 2 Human Binding pKi = 8.3 8.3 - 1
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 9138 None 2 Human Binding pKi = 8.3 8.3 - 1
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 75879 None 20 Human Binding pKi = 8.3 8.3 43 2
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 75879 None 20 Human Binding pKi = 8.3 8.3 43 2
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 167494 None 0 Human Binding pKi = 7.3 7.3 - 1
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 167494 None 0 Human Binding pKi = 7.3 7.3 - 1
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 111735 None 0 Human Binding pKi = 7.3 7.3 - 1
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 111735 None 0 Human Binding pKi = 7.3 7.3 - 1
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 69038 None 0 Human Binding pKi = 6.3 6.3 - 1
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 69038 None 0 Human Binding pKi = 6.3 6.3 - 1
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 89904 None 0 Human Binding pKi = 5.3 5.3 - 1
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 89904 None 0 Human Binding pKi = 5.3 5.3 - 1
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 75870 None 0 Human Binding pKi = 7.3 7.3 - 1
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 75870 None 0 Human Binding pKi = 7.3 7.3 - 1
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 175662 None 0 Human Binding pKi = 7.3 7.3 - 1
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 175662 None 0 Human Binding pKi = 7.3 7.3 - 1
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 69062 None 0 Human Binding pKi = 7.3 7.3 - 1
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 69062 None 0 Human Binding pKi = 7.3 7.3 - 1
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 183084 None 0 Human Binding pKi = 7.3 7.3 - 1
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 183084 None 0 Human Binding pKi = 7.3 7.3 - 1
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 69067 None 0 Human Binding pKi = 7.2 7.2 - 1
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 69067 None 0 Human Binding pKi = 7.2 7.2 - 1
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 69037 None 0 Human Binding pKi = 6.2 6.2 - 1
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 69037 None 0 Human Binding pKi = 6.2 6.2 - 1
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 139660 None 0 Human Binding pKi = 7.2 7.2 - 1
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 139660 None 0 Human Binding pKi = 7.2 7.2 - 1
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 208466 None 38 Human Binding pKi = 8.2 8.2 - 1
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 69048 None 0 Human Binding pKi = 8.2 8.2 - 1
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 69048 None 0 Human Binding pKi = 8.2 8.2 - 1
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 179939 None 0 Human Binding pKi = 8.2 8.2 - 1
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 179939 None 0 Human Binding pKi = 8.2 8.2 - 1
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 182312 None 0 Human Binding pKi = 8.2 8.2 - 1
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 182312 None 0 Human Binding pKi = 8.2 8.2 - 1
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 183302 None 0 Human Binding pKi = 8.2 8.2 - 1
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 183302 None 0 Human Binding pKi = 8.2 8.2 - 1
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 92271 None 0 Human Binding pKi = 8.2 8.2 1548 2
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 92271 None 0 Human Binding pKi = 8.2 8.2 1548 2
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 92271 None 0 Human Binding pKi = 8.2 8.2 1548 2
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 92271 None 0 Human Binding pKi = 8.2 8.2 1548 2
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 69034 None 0 Human Binding pKi = 8.2 8.2 - 1
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 69034 None 0 Human Binding pKi = 8.2 8.2 - 1
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 117186 None 0 Human Binding pKi = 8.2 8.2 - 1
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 117186 None 0 Human Binding pKi = 8.2 8.2 - 1
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 173947 None 0 Human Binding pKi = 8.2 8.2 - 1
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 173947 None 0 Human Binding pKi = 8.2 8.2 - 1
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 71283 None 0 Human Binding pKi = 8.2 8.2 - 1
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 71283 None 0 Human Binding pKi = 8.2 8.2 - 1
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 180052 None 0 Human Binding pKi = 8.2 8.2 - 1
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 180052 None 0 Human Binding pKi = 8.2 8.2 - 1
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 3063 None 35 Human Binding pKi = 8.2 8.2 1 3
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 3063 None 35 Human Binding pKi = 8.2 8.2 1 3
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 3063 None 35 Human Binding pKi = 8.2 8.2 1 3
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 3063 None 35 Human Binding pKi = 8.2 8.2 1 3
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 3063 None 35 Human Binding pKi = 8.2 8.2 1 3
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 3063 None 35 Human Binding pKi = 8.2 8.2 1 3
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 3063 None 35 Human Binding pKi = 8.2 8.2 1 3
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 3063 None 35 Human Binding pKi = 8.2 8.2 1 3
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 111732 None 0 Human Binding pKi = 8.2 8.2 - 1
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 111732 None 0 Human Binding pKi = 8.2 8.2 - 1
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 71269 None 0 Human Binding pKi = 8.2 8.2 - 1
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 71269 None 0 Human Binding pKi = 8.2 8.2 - 1
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 92271 None 0 Human Binding pKi = 8.2 8.2 1548 2
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 92271 None 0 Human Binding pKi = 8.2 8.2 1548 2
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 69068 None 0 Human Binding pKi = 7.2 7.2 - 1
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 69068 None 0 Human Binding pKi = 7.2 7.2 - 1
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 181349 None 0 Human Binding pKi = 6.2 6.2 - 1
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 181349 None 0 Human Binding pKi = 6.2 6.2 - 1
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 139938 None 0 Human Binding pKi = 7.2 7.2 - 1
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 139938 None 0 Human Binding pKi = 7.2 7.2 - 1
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 139975 None 0 Human Binding pKi = 7.2 7.2 - 1
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 139975 None 0 Human Binding pKi = 7.2 7.2 - 1
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 2232 None 24 Human Binding pKi = 7.2 7.2 - 1
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 2232 None 24 Human Binding pKi = 7.2 7.2 - 1
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 2232 None 24 Human Binding pKi = 7.2 7.2 - 1
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 182377 None 0 Human Binding pKi = 7.2 7.2 - 1
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 182377 None 0 Human Binding pKi = 7.2 7.2 - 1
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 146034 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146034 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 181986 None 0 Human Binding pKi = 7.2 7.2 - 1
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 181986 None 0 Human Binding pKi = 7.2 7.2 - 1
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 69015 None 0 Human Binding pKi = 6.2 6.2 - 1
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 69015 None 0 Human Binding pKi = 6.2 6.2 - 1
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 69011 None 0 Human Binding pKi = 7.2 7.2 - 1
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 69011 None 0 Human Binding pKi = 7.2 7.2 - 1
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 166499 None 0 Human Binding pKi = 6.2 6.2 -239 5
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 166499 None 0 Human Binding pKi = 6.2 6.2 -239 5
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 75878 None 0 Human Binding pKi = 7.2 7.2 - 1
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 75878 None 0 Human Binding pKi = 7.2 7.2 - 1
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 111734 None 0 Human Binding pKi = 7.2 7.2 - 1
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 111734 None 0 Human Binding pKi = 7.2 7.2 - 1
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 75879 None 20 Human Binding pKi = 8.2 8.2 43 2
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 75879 None 20 Human Binding pKi = 8.2 8.2 43 2
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 69051 None 0 Human Binding pKi = 8.2 8.2 - 1
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 69051 None 0 Human Binding pKi = 8.2 8.2 - 1
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 9725 None 33 Human Binding pKi = 8.2 8.2 - 1
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 9725 None 33 Human Binding pKi = 8.2 8.2 - 1
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 69050 None 0 Human Binding pKi = 8.1 8.1 - 1
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 69050 None 0 Human Binding pKi = 8.1 8.1 - 1
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 92278 None 0 Human Binding pKi = 8.1 8.1 - 1
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 92278 None 0 Human Binding pKi = 8.1 8.1 - 1
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 148180 None 0 Human Binding pKi = 6.1 6.1 -1023 8
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 148180 None 0 Human Binding pKi = 6.1 6.1 -1023 8
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 69053 None 0 Human Binding pKi = 7.1 7.1 - 1
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 69053 None 0 Human Binding pKi = 7.1 7.1 - 1
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 214133 None 23 Human Binding pKi = 7.1 7.1 - 1
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 69060 None 0 Human Binding pKi = 7.1 7.1 - 1
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 69060 None 0 Human Binding pKi = 7.1 7.1 - 1
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 89072 None 0 Human Binding pKi = 6.1 6.1 - 1
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 89072 None 0 Human Binding pKi = 6.1 6.1 - 1
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 139778 None 0 Human Binding pKi = 8.1 8.1 - 1
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 139778 None 0 Human Binding pKi = 8.1 8.1 - 1
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 125192 None 0 Human Binding pKi = 8.1 8.1 - 1
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 125192 None 0 Human Binding pKi = 8.1 8.1 - 1
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 81839 None 0 Human Binding pKi = 8.1 8.1 - 1
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 81839 None 0 Human Binding pKi = 8.1 8.1 - 1
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 181039 None 0 Human Binding pKi = 8.1 8.1 - 1
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 181039 None 0 Human Binding pKi = 8.1 8.1 - 1
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 69059 None 0 Human Binding pKi = 7.1 7.1 - 1
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 69059 None 0 Human Binding pKi = 7.1 7.1 - 1
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 88489 None 0 Human Binding pKi = 6.1 6.1 - 1
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 88489 None 0 Human Binding pKi = 6.1 6.1 - 1
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 92281 None 0 Human Binding pKi = 7.1 7.1 - 1
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 92281 None 0 Human Binding pKi = 7.1 7.1 - 1
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 69010 None 0 Human Binding pKi = 7.1 7.1 - 1
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 69010 None 0 Human Binding pKi = 7.1 7.1 - 1
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 67519 None 3 Human Binding pKi = 6.1 6.1 - 1
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 67519 None 3 Human Binding pKi = 6.1 6.1 - 1
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 69061 None 0 Human Binding pKi = 8.1 8.1 - 1
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 69061 None 0 Human Binding pKi = 8.1 8.1 - 1
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 125190 None 0 Human Binding pKi = 8.1 8.1 - 1
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 125190 None 0 Human Binding pKi = 8.1 8.1 - 1
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 139860 None 0 Human Binding pKi = 8.1 8.1 - 1
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 139860 None 0 Human Binding pKi = 8.1 8.1 - 1
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 183571 None 0 Human Binding pKi = 8.1 8.1 - 1
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 183571 None 0 Human Binding pKi = 8.1 8.1 - 1
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 92279 None 0 Human Binding pKi = 8.0 8.0 - 1
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 92279 None 0 Human Binding pKi = 8.0 8.0 - 1
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 92281 None 0 Human Binding pKi = 8.0 8.0 - 1
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 92281 None 0 Human Binding pKi = 8.0 8.0 - 1
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 92281 None 0 Human Binding pKi = 8.0 8.0 - 1
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 92281 None 0 Human Binding pKi = 8.0 8.0 - 1
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 117190 None 0 Human Binding pKi = 8.0 8.0 - 1
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 117190 None 0 Human Binding pKi = 8.0 8.0 - 1
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 180858 None 0 Human Binding pKi = 8.0 8.0 - 1
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 180858 None 0 Human Binding pKi = 8.0 8.0 - 1
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 184079 None 0 Human Binding pKi = 7.1 7.1 - 1
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 184079 None 0 Human Binding pKi = 7.1 7.1 - 1
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 66815 None 0 Human Binding pKi = 6.0 6.0 - 1
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 66815 None 0 Human Binding pKi = 6.0 6.0 - 1
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 183387 None 0 Human Binding pKi = 7.0 7.0 - 1
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 183387 None 0 Human Binding pKi = 7.0 7.0 - 1
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 146281 None 0 Human Binding pKi = 6.0 6.0 - 1
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 146281 None 0 Human Binding pKi = 6.0 6.0 - 1
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 2451 None 20 Human Binding pIC50 = 8.1 8.1 - 0
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 2451 None 20 Human Binding pIC50 = 8.1 8.1 - 0
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 2451 None 20 Human Binding pIC50 = 8.1 8.1 - 0
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 2451 None 20 Human Binding pIC50 = 8.1 8.1 - 0
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 2451 None 20 Human Binding pIC50 = 7.8 7.8 - 0
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 2451 None 20 Human Binding pIC50 = 7.8 7.8 - 0
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 2451 None 20 Human Binding pIC50 = 7.8 7.8 - 0
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 2451 None 20 Human Binding pIC50 = 7.8 7.8 - 0
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 1320 None 0 Human Binding pKd = 7.4 7.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12907757
1093 1792 None 0 Human Binding pKd = 7.7 7.7 -12 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
1093 1792 None 0 Human Binding pKd = 7.7 7.7 -12 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
4345065 1792 None 0 Human Binding pKd = 7.7 7.7 -12 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
4345065 1792 None 0 Human Binding pKd = 7.7 7.7 -12 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
1100 1606 None 45 Human Binding pKd = 7.9 7.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11061542
6918297 1606 None 45 Human Binding pKd = 7.9 7.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11061542
CHEMBL108335 1606 None 45 Human Binding pKd = 7.9 7.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11061542
1099 1784 None 0 Human Binding pKd = 9.0 9.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12907757
1099 1784 None 0 Human Binding pKd = 9.0 9.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
1092 3156 None 0 Rat Binding pKi = 8.0 8.0 - 1
NoneNone
Drug Central None None None None None
134715446 3156 None 0 Rat Binding pKi = 8.0 8.0 - 1
NoneNone
Drug Central None None None None None
2232 3156 None 0 Rat Binding pKi = 8.0 8.0 - 1
NoneNone
Drug Central None None None None None
6918245 3156 None 0 Rat Binding pKi = 8.0 8.0 - 1
NoneNone
Drug Central None None None None None
CHEMBL106593 3156 None 0 Rat Binding pKi = 8.0 8.0 - 1
NoneNone
Drug Central None None None None None
58438464 3063 None 35 Mouse Binding pKi = 8.1 8.1 -2 3
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 3063 None 35 Mouse Binding pKi = 8.1 8.1 -2 3
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 3063 None 35 Mouse Binding pKi = 8.1 8.1 -2 3
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 3063 None 35 Mouse Binding pKi = 8.1 8.1 -2 3
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 3063 None 35 Rat Binding pKi = 8.5 8.5 -1 3
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 3063 None 35 Rat Binding pKi = 8.5 8.5 -1 3
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 3063 None 35 Rat Binding pKi = 8.5 8.5 -1 3
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 3063 None 35 Rat Binding pKi = 8.5 8.5 -1 3
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 3063 None 35 Human Binding pKi = 8.9 8.9 1 3
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 3063 None 35 Human Binding pKi = 8.9 8.9 1 3
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 3063 None 35 Human Binding pKi = 8.9 8.9 1 3
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 3063 None 35 Human Binding pKi = 8.9 8.9 1 3
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 3068 None 0 Rat Binding pKi = 6.6 6.6 -3 2
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 3068 None 0 Rat Binding pKi = 6.6 6.6 -3 2
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 3068 None 0 Human Binding pKi = 7.1 7.1 3 2
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 3068 None 0 Human Binding pKi = 7.1 7.1 3 2
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 4110 None 23 Human Binding pKi = 7.8 7.8 - 1
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 4110 None 23 Human Binding pKi = 7.8 7.8 - 1
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 4110 None 23 Human Binding pKi = 7.8 7.8 - 1
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 1390 None 0 Rat Binding pKi = 7.9 7.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11314756
1098 1390 None 0 Rat Binding pKi = 7.9 7.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14763915
1101 656 None 0 Human Binding pKi = 8.1 8.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15339248
10740 1936 None 0 Human Binding pKi = 8.9 8.9 - 1
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 1936 None 0 Human Binding pKi = 8.9 8.9 - 1
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 3156 None 0 Rat Binding pKi = 9.3 9.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
134715446 3156 None 0 Rat Binding pKi = 9.3 9.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
2232 3156 None 0 Rat Binding pKi = 9.3 9.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
6918245 3156 None 0 Rat Binding pKi = 9.3 9.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
CHEMBL106593 3156 None 0 Rat Binding pKi = 9.3 9.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
178024 1969 None 33 Human Binding pKi = 9.3 9.3 - 1
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 1969 None 33 Human Binding pKi = 9.3 9.3 - 1
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 1969 None 33 Human Binding pKi = 9.3 9.3 - 1
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 1784 None 0 Human Binding pKi None 8.0 8.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11314756
1093 1792 None 0 Rat Binding pKi None 8.8 8.8 12 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
4345065 1792 None 0 Rat Binding pKi None 8.8 8.8 12 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793