Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
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name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
44570962 183833 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 435 4 1 5 2.5 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL480821 183833 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 435 4 1 5 2.5 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
145950336 162803 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 3 3 3.1 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4172656 162803 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 3 3 3.1 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.8b00322
156016416 177633 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 6 3 5 3.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641513 177633 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 6 3 5 3.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
16752684 94470 1 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 484 5 1 7 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL251572 94470 1 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 484 5 1 7 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
156014430 177199 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4635542 177199 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
156016416 177633 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 6 3 5 3.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641513 177633 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 6 3 5 3.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
16752684 94470 1 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 484 5 1 7 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2008.12.042
CHEMBL251572 94470 1 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 484 5 1 7 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2008.12.042
44570963 183856 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 435 4 1 5 2.5 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL481013 183856 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 435 4 1 5 2.5 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
156014430 177199 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4635542 177199 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
44444563 154931 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 478 5 1 6 3.7 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)cc1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL401134 154931 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 478 5 1 6 3.7 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)cc1)CC2 10.1016/j.bmcl.2007.09.067
156011926 177376 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 6 4 5 2.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4638297 177376 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 6 4 5 2.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
44571002 191074 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 437 4 2 6 1.1 Cc1ccc(-c2ccc(S(=O)(=O)N3CC[C@H](O)[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL518774 191074 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 437 4 2 6 1.1 Cc1ccc(-c2ccc(S(=O)(=O)N3CC[C@H](O)[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
44449987 95864 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 493 16 4 10 0.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCSCCO 10.1016/j.bmcl.2008.03.059
CHEMBL259166 95864 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 493 16 4 10 0.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCSCCO 10.1016/j.bmcl.2008.03.059
25010378 159374 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 525 16 4 11 -0.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCS(=O)(=O)CCO 10.1016/j.bmcl.2008.03.059
CHEMBL410074 159374 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 525 16 4 11 -0.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCS(=O)(=O)CCO 10.1016/j.bmcl.2008.03.059
44449955 159388 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 509 14 4 9 1.6 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1cccc(O)c1 10.1016/j.bmcl.2008.03.059
CHEMBL410085 159388 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 509 14 4 9 1.6 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1cccc(O)c1 10.1016/j.bmcl.2008.03.059
156011926 177376 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 6 4 5 2.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4638297 177376 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 6 4 5 2.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4Cl)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
156017918 177782 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 591 7 3 7 2.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4643530 177782 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 591 7 3 7 2.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2Cl)on1 10.1021/acs.jmedchem.0c00828
156015100 177548 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4640507 177548 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
156017918 177782 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 591 7 3 7 2.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4643530 177782 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 591 7 3 7 2.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2Cl)on1 10.1021/acs.jmedchem.0c00828
44570960 183964 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 417 4 1 5 2.4 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2)o1 10.1016/j.bmcl.2008.12.042
CHEMBL481796 183964 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 417 4 1 5 2.4 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2)o1 10.1016/j.bmcl.2008.12.042
24894012 176773 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 497 14 4 9 1.6 CC(C)(N)C(=O)N[C@H](CCC(F)(F)c1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.05.100
CHEMBL460680 176773 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 497 14 4 9 1.6 CC(C)(N)C(=O)N[C@H](CCC(F)(F)c1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.05.100
156015100 177548 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4640507 177548 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
44437979 10295 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 655 12 5 5 4.1 NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)c1ccccc1 10.1016/j.bmc.2007.01.057
CHEMBL1162065 10295 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 655 12 5 5 4.1 NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)c1ccccc1 10.1016/j.bmc.2007.01.057
44437979 10295 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 655 12 5 5 4.1 NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)c1ccccc1 10.1016/j.bmc.2007.01.057
CHEMBL1162065 10295 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 655 12 5 5 4.1 NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)c1ccccc1 10.1016/j.bmc.2007.01.057
44454303 97541 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
CHEMBL270666 97541 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
156020725 178081 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647963 178081 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
44570764 184025 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 481 4 1 4 3.8 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3cc(Cl)ccc3Cl)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL482220 184025 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 481 4 1 4 3.8 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3cc(Cl)ccc3Cl)cc2)C1 10.1016/j.bmcl.2008.12.042
24803512 88978 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1Cl 10.6019/CHEMBL2364335
CHEMBL2364468 88978 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1Cl 10.6019/CHEMBL2364335
156020725 178081 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647963 178081 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
9917957 109691 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Compound was evaluated for GH release for effect on human GH secretagogue receptorCompound was evaluated for GH release for effect on human GH secretagogue receptor
ChEMBL 683 14 4 5 4.3 NC(=O)CN(CCc1ccccc1)C(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1 10.1021/jm970342o
CHEMBL322912 109691 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Compound was evaluated for GH release for effect on human GH secretagogue receptorCompound was evaluated for GH release for effect on human GH secretagogue receptor
ChEMBL 683 14 4 5 4.3 NC(=O)CN(CCc1ccccc1)C(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1 10.1021/jm970342o
44447855 194833 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 539 15 4 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1-c1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL539929 194833 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 539 15 4 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1-c1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
178024 1958 33 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
5867 1958 33 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
CHEMBL13817 1958 33 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
156013414 177448 6 None 1905 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4639111 177448 6 None 1905 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
156013297 177460 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639229 177460 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
44452749 96186 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 499 7 2 6 4.5 COc1ccc(F)c(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)cc2)c1 10.1016/j.bmcl.2007.12.021
CHEMBL260819 96186 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 499 7 2 6 4.5 COc1ccc(F)c(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)cc2)c1 10.1016/j.bmcl.2007.12.021
44570765 191416 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 421 4 1 5 2.1 Cc1ccc(-c2ccc(S(=O)(=O)N3CCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL519301 191416 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 421 4 1 5 2.1 Cc1ccc(-c2ccc(S(=O)(=O)N3CCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
59007047 88936 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 6 5.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)cc1C 10.6019/CHEMBL2364335
CHEMBL2364427 88936 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 6 5.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)cc1C 10.6019/CHEMBL2364335
178024 1958 33 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
5867 1958 33 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
CHEMBL13817 1958 33 None -1 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
25022640 97773 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
CHEMBL271876 97773 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
44454337 155579 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL404545 155579 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
44447839 94962 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 499 14 4 10 0.6 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)cc1F)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254765 94962 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 499 14 4 10 0.6 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)cc1F)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
156013414 177448 6 None 1905 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4639111 177448 6 None 1905 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
156013297 177460 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639229 177460 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@H]3CCCN(C)C3)cc2c1 10.1021/acs.jmedchem.0c00828
44447857 166852 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 497 14 4 10 0.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1Cl)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL428592 166852 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 497 14 4 10 0.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1Cl)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
156019724 177967 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4646219 177967 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
22888474 63434 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 525 9 1 6 5.6 COc1cccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)c1 10.1016/j.bmcl.2005.02.040
CHEMBL179823 63434 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 525 9 1 6 5.6 COc1cccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)c1 10.1016/j.bmcl.2005.02.040
11306502 63612 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180094 63612 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
11306502 63612 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180094 63612 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
11306502 63612 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180094 63612 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
22888476 122792 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 525 9 1 6 5.6 COc1ccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
CHEMBL360547 122792 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 525 9 1 6 5.6 COc1ccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
22888476 122792 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 525 9 1 6 5.6 COc1ccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
CHEMBL360547 122792 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 525 9 1 6 5.6 COc1ccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
44454117 155532 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
CHEMBL404336 155532 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
44444559 94407 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 451 4 1 5 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc3ccccc3c1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL251169 94407 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 451 4 1 5 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc3ccccc3c1)CC2 10.1016/j.bmcl.2007.09.067
156011750 177266 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccccc2Cl)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4636502 177266 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccccc2Cl)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
156019724 177967 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4646219 177967 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 5 2.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3C)cc2c1 10.1021/acs.jmedchem.0c00828
44453123 97958 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 503 6 2 5 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(Cl)ccc2F)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL272753 97958 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 503 6 2 5 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(Cl)ccc2F)cc1 10.1016/j.bmcl.2007.12.021
44570966 183545 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 437 4 2 6 1.1 Cc1ccc(-c2ccc(S(=O)(=O)N3C[C@H](O)C[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL480037 183545 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 437 4 2 6 1.1 Cc1ccc(-c2ccc(S(=O)(=O)N3C[C@H](O)C[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
59007062 88938 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)cc1F 10.6019/CHEMBL2364335
CHEMBL2364429 88938 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)cc1F 10.6019/CHEMBL2364335
24803514 88983 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1Cl 10.6019/CHEMBL2364335
CHEMBL2364472 88983 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1Cl 10.6019/CHEMBL2364335
44447852 155538 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 477 14 4 10 0.6 Cc1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL404354 155538 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 477 14 4 10 0.6 Cc1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
156011750 177266 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccccc2Cl)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4636502 177266 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccccc2Cl)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
44450016 160536 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 489 17 4 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL411259 160536 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 489 17 4 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCCCO 10.1016/j.bmcl.2008.03.059
44454367 95232 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
CHEMBL256235 95232 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
22867441 10283 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161835 10283 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1016/j.bmc.2007.01.057
16114096 79131 1 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)c(OC)c1 10.1021/jm0704550
CHEMBL2113324 79131 1 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)c(OC)c1 10.1021/jm0704550
22867441 10283 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161835 10283 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1016/j.bmc.2007.01.057
44447841 155054 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.6 CC(C)(N)C(=O)N[C@H](COCc1cccc(Cl)c1Cl)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL401827 155054 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.6 CC(C)(N)C(=O)N[C@H](COCc1cccc(Cl)c1Cl)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
69195371 88862 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 472 6 2 7 4.1 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)n3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364354 88862 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 472 6 2 7 4.1 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)n3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
44450101 159436 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 495 13 4 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCNC(=O)CCc1cccc(O)c1 10.1016/j.bmcl.2008.03.059
CHEMBL410135 159436 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 495 13 4 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCNC(=O)CCc1cccc(O)c1 10.1016/j.bmcl.2008.03.059
44391039 131762 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 540 9 1 7 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3cccc([N+](=O)[O-])c3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL369329 131762 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 540 9 1 7 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3cccc([N+](=O)[O-])c3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44449988 161077 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 477 16 4 10 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCOCCO 10.1016/j.bmcl.2008.03.059
CHEMBL411697 161077 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 477 16 4 10 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCOCCO 10.1016/j.bmcl.2008.03.059
44447843 94991 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1C(F)(F)F)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254973 94991 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1C(F)(F)F)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
10280020 63062 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 529 8 1 5 6.2 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccc(Cl)cc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL178900 63062 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 529 8 1 5 6.2 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccc(Cl)cc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
156021297 178065 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647797 178065 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44444571 93950 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 498 5 1 7 4.1 COc1cc2c(cc1N1C[C@H](C)NC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL248544 93950 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 498 5 1 7 4.1 COc1cc2c(cc1N1C[C@H](C)NC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
10553921 104533 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 517 9 4 4 2.9 CCNC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
CHEMBL310457 104533 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 517 9 4 4 2.9 CCNC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
10345516 139250 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1016/j.bmc.2007.01.057
CHEMBL379074 139250 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1016/j.bmc.2007.01.057
156012122 177357 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637980 177357 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156021297 178065 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647797 178065 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
11584048 98001 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1Cl 10.1016/j.bmcl.2007.12.021
CHEMBL272993 98001 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1Cl 10.1016/j.bmcl.2007.12.021
24755624 157276 2 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL407706 157276 2 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1 10.1016/j.bmcl.2007.12.021
24755624 157276 2 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1 10.1016/j.bmcl.2008.12.042
CHEMBL407706 157276 2 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1 10.1016/j.bmcl.2008.12.042
69197353 88916 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(NS(=O)(=O)c2ccc(-c3cc(C)cs3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364408 88916 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(NS(=O)(=O)c2ccc(-c3cc(C)cs3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
44454060 155308 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL403180 155308 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
10553921 104533 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 517 9 4 4 2.9 CCNC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
CHEMBL310457 104533 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 517 9 4 4 2.9 CCNC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
10345516 139250 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1016/j.bmc.2007.01.057
CHEMBL379074 139250 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1016/j.bmc.2007.01.057
127047525 139742 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 858 20 7 9 5.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798559 139742 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 858 20 7 9 5.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
156022162 178182 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 8 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)NC[C@@H]1CCCN1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4649634 178182 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 8 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)NC[C@@H]1CCCN1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
156012122 177357 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637980 177357 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
20600693 63426 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 566 11 1 6 4.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C(=O)N(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL179785 63426 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 566 11 1 6 4.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C(=O)N(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44560945 179078 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 391 9 2 7 2.1 CC(C)(N)C(=O)N[C@H](CCC(F)(F)c1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.05.100
CHEMBL471751 179078 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 391 9 2 7 2.1 CC(C)(N)C(=O)N[C@H](CCC(F)(F)c1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.05.100
216208 9695 33 None -5 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
CHEMBL113313 9695 33 None -5 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
44449891 96445 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 539 16 4 10 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1ccccc1C(=O)NCCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL262358 96445 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 539 16 4 10 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1ccccc1C(=O)NCCCCO 10.1016/j.bmcl.2008.03.059
216208 9695 33 None -5 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
CHEMBL113313 9695 33 None -5 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
156021478 178031 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 7 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647258 178031 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 7 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3)cc2c1 10.1021/acs.jmedchem.0c00828
44437955 10293 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 534 11 4 6 2.6 NCC(O)CNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCCN1C(=O)CCSc2ccccc21 10.1016/j.bmc.2007.01.057
CHEMBL1162063 10293 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 534 11 4 6 2.6 NCC(O)CNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCCN1C(=O)CCSc2ccccc21 10.1016/j.bmc.2007.01.057
9807597 182993 5 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 513 7 4 4 3.5 CNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1016/j.bmc.2007.01.057
CHEMBL47938 182993 5 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 513 7 4 4 3.5 CNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1016/j.bmc.2007.01.057
156018364 177889 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645148 177889 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156021478 178031 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 7 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647258 178031 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 7 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NC[C@H]3CCCN3)cc2c1 10.1021/acs.jmedchem.0c00828
156022090 178179 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4649603 178179 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
156022162 178182 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 8 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)NC[C@@H]1CCCN1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4649634 178182 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 8 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)NC[C@@H]1CCCN1)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
56926175 68984 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL1923504 68984 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
56926356 68990 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O nan
CHEMBL1923512 68990 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O nan
56926461 69007 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923609 69007 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926462 69008 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923610 69008 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
57399248 69015 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923617 69015 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
11664206 69024 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923626 69024 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
56926894 69035 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
CHEMBL1923638 69035 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
11526745 69039 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923642 69039 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C nan
11526696 71573 17 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
CHEMBL1923502 71573 17 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
CHEMBL1963249 71573 17 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
134130631 142348 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 576 5 4 6 3.4 COc1ccc(C[C@@H]2NC(=O)C3(CCCC3)NC(=O)[C@H](CC(C)C)NCCOc3ccccc3/C=C\CNC2=O)cc1 nan
CHEMBL3889512 142348 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 576 5 4 6 3.4 COc1ccc(C[C@@H]2NC(=O)C3(CCCC3)NC(=O)[C@H](CC(C)C)NCCOc3ccccc3/C=C\CNC2=O)cc1 nan
134137202 142801 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 552 5 3 6 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3893048 142801 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 552 5 3 6 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134137257 143112 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 540 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3895776 143112 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 540 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134133518 143428 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 552 2 4 5 3.4 CC1(C)NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
CHEMBL3898348 143428 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 552 2 4 5 3.4 CC1(C)NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
134133352 143480 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3898794 143480 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@@H](C)N(C)C1=O nan
134134286 143669 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 598 5 3 5 4.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3900284 143669 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 598 5 3 5 4.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(-c3ccccc3)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134135712 144113 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 533 4 4 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN(C)C1=O nan
CHEMBL3903845 144113 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 533 4 4 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN(C)C1=O nan
11512561 144344 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 574 3 3 5 3.4 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2Cl)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3905791 144344 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 574 3 3 5 3.4 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2Cl)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134133037 144542 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3907497 144542 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](C)N(C)C1=O nan
134132893 144838 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 4 4 6 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3909834 144838 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 4 4 6 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134132152 144907 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3910300 144907 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@@H](C)N(C)C1=O nan
134142218 145262 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 564 4 4 5 3.5 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3913052 145262 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 564 4 4 5 3.5 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)C2(CCCC2)NC1=O nan
134142433 145301 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 534 3 4 6 1.8 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOC2)NC1=O nan
CHEMBL3913335 145301 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 534 3 4 6 1.8 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOC2)NC1=O nan
134142839 145361 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3913855 145361 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134143635 145549 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2Cl)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3915269 145549 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2Cl)NC(=O)C2(CCCC2)NC1=O nan
134143366 145735 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 578 4 4 4 4.6 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3916659 145735 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 578 4 4 4 4.6 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134142204 145912 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3918046 145912 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
11584702 146166 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 540 3 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3920049 146166 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 540 3 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134140270 146348 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 536 4 3 5 3.1 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3921499 146348 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 536 4 3 5 3.1 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134139279 146422 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 594 4 4 5 4.1 CCC(C)[C@H]1NCCOc2ccccc2[C@H]2C[C@@H]2CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3922056 146422 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 594 4 4 5 4.1 CCC(C)[C@H]1NCCOc2ccccc2[C@H]2C[C@@H]2CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134139286 146529 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3922810 146529 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCCC2)NC1=O nan
134141886 147093 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 546 4 4 5 3.4 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3927481 147093 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 546 4 4 5 3.4 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
117812380 147727 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 617 5 4 7 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(NS(C)(=O)=O)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3932408 147727 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 617 5 4 7 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(NS(C)(=O)=O)ccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134138595 147730 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 544 2 4 5 3.3 O=C1NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccccc1 nan
CHEMBL3932434 147730 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 544 2 4 5 3.3 O=C1NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccccc1 nan
134138824 147990 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 525 3 3 6 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ncccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3934402 147990 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 525 3 3 6 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ncccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134148504 148330 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 518 4 3 4 3.4 CC[C@H](C)[C@@H]1NCc2ccccc2C/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3937200 148330 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 518 4 3 4 3.4 CC[C@H](C)[C@@H]1NCc2ccccc2C/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134149306 148450 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 3 3 5 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCC#Cc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3938104 148450 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 3 3 5 1.6 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCC#Cc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134145791 148762 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 596 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2c(F)c(F)c(F)c(F)c2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3940705 148762 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 596 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2c(F)c(F)c(F)c(F)c2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134145564 149066 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 518 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3943086 149066 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 518 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134147441 149465 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 2 4 5 3.0 C[C@H]1NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
CHEMBL3946348 149465 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 2 4 5 3.0 C[C@H]1NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O nan
134155239 150990 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 564 3 4 5 3.4 O=C1NC/C=C\c2ccccc2OCCN[C@@H](C2CC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccc(Cl)cc1 nan
CHEMBL3958460 150990 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 564 3 4 5 3.4 O=C1NC/C=C\c2ccccc2OCCN[C@@H](C2CC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccc(Cl)cc1 nan
134155132 151068 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 502 4 3 5 2.9 CC[C@H](C)[C@]1(C)NCCOc2ccccc2CCCNC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3959108 151068 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 502 4 3 5 2.9 CC[C@H](C)[C@]1(C)NCCOc2ccccc2CCCNC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](C)N(C)C1=O nan
134154079 152379 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 512 4 4 5 3.2 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](CC(C)C)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3970499 152379 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 512 4 4 5 3.2 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](CC(C)C)NC(=O)C2(CCCC2)NC1=O nan
134153247 152696 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 582 4 4 6 2.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCOC2)NC1=O nan
CHEMBL3973085 152696 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 582 4 4 6 2.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C2(CCOC2)NC1=O nan
44570763 190235 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 449 4 1 4 2.7 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3cc(F)ccc3F)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL517543 190235 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 449 4 1 4 2.7 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3cc(F)ccc3F)cc2)C1 10.1016/j.bmcl.2008.12.042
9890504 89711 0 None - 1 Human 9.0 pEC50 = 9 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 461 10 3 10 -0.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)N1CC[C@@H](O)C1 10.1021/jm7010595
CHEMBL237699 89711 0 None - 1 Human 9.0 pEC50 = 9 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 461 10 3 10 -0.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)N1CC[C@@H](O)C1 10.1021/jm7010595
24969109 88846 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 444 5 2 6 3.8 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cccc(N4C[C@H](C)N[C@H](C)C4)n3)cc2F)o1 10.6019/CHEMBL2364335
CHEMBL2364338 88846 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 444 5 2 6 3.8 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cccc(N4C[C@H](C)N[C@H](C)C4)n3)cc2F)o1 10.6019/CHEMBL2364335
11518200 88861 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364353 88861 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11641108 88890 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364382 88890 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69197887 88911 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2C)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364403 88911 0 None - 1 Human 9.0 pEC50 = 9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2C)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
44447856 161790 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 558 15 4 12 1.6 Cc1noc(C)c1-c1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL414394 161790 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 558 15 4 12 1.6 Cc1noc(C)c1-c1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
156018364 177889 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645148 177889 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156022090 178179 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4649603 178179 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
10323604 10277 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161828 10277 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
10323604 10277 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161828 10277 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
44447853 94935 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 493 15 4 11 0.3 COc1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254565 94935 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 493 15 4 11 0.3 COc1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
25022503 155539 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 540 15 4 11 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1-c1cccnc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL404355 155539 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 540 15 4 11 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1-c1cccnc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44269035 27301 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 490 5 4 5 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CC(O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
CHEMBL13675 27301 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 490 5 4 5 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CC(O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
44269039 98313 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@@]2(CC(=O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
CHEMBL275093 98313 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@@]2(CC(=O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
145956061 162669 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4170481 162669 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
44570965 189813 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 418 4 2 6 0.8 Cc1ccc(-c2ccc(S(=O)(=O)N3CCNC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2)o1 10.1016/j.bmcl.2008.12.042
CHEMBL516602 189813 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 418 4 2 6 0.8 Cc1ccc(-c2ccc(S(=O)(=O)N3CCNC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2)o1 10.1016/j.bmcl.2008.12.042
69194933 88933 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 455 5 2 5 5.0 Cc1csc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3C)cc2)c1 10.6019/CHEMBL2364335
CHEMBL2364424 88933 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 455 5 2 5 5.0 Cc1csc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3C)cc2)c1 10.6019/CHEMBL2364335
69198297 88942 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cc(C)cs3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364432 88942 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cc(C)cs3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
44447850 94906 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 488 14 4 11 0.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1C#N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254363 94906 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 488 14 4 11 0.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1C#N)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44450015 96289 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 475 16 4 9 0.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL261358 96289 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 475 16 4 9 0.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCCO 10.1016/j.bmcl.2008.03.059
178024 1958 33 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/j.bmc.2007.01.057
5867 1958 33 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/j.bmc.2007.01.057
CHEMBL13817 1958 33 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/j.bmc.2007.01.057
178024 1958 33 None 1 3 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(97)10199-8
5867 1958 33 None 1 3 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(97)10199-8
CHEMBL13817 1958 33 None 1 3 Rat 8.9 pEC50 = 8.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(97)10199-8
178024 1958 33 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/j.bmc.2007.01.057
5867 1958 33 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/j.bmc.2007.01.057
CHEMBL13817 1958 33 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/j.bmc.2007.01.057
145956061 162669 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4170481 162669 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
44450104 95772 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 496 14 4 10 -1.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCS(N)(=O)=O 10.1016/j.bmcl.2008.03.059
CHEMBL258761 95772 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 496 14 4 10 -1.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCS(N)(=O)=O 10.1016/j.bmcl.2008.03.059
CHEMBL500468 214092 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/j.bmcl.2008.03.059
CHEMBL500468 214092 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1021/jm300414b
22888475 63795 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 523 9 1 6 5.4 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccc(C=O)cc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180246 63795 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 523 9 1 6 5.4 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccc(C=O)cc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL500468 214092 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/j.bmcl.2005.02.040
162653916 180521 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 707 15 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4753794 180521 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 707 15 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL500468 214092 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/j.bmcl.2008.02.021
CHEMBL500468 214092 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/j.bmcl.2008.05.100
178024 1958 33 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(01)00324-9
5867 1958 33 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(01)00324-9
CHEMBL13817 1958 33 None -1 3 Human 8.9 pEC50 = 8.9 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(01)00324-9
156012849 177274 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4636571 177274 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44390996 64274 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 563 8 1 5 6.6 CC(C)N(CCNC(=O)C1c2ccc(Oc3cccc(C(F)(F)F)c3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181063 64274 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 563 8 1 5 6.6 CC(C)N(CCNC(=O)C1c2ccc(Oc3cccc(C(F)(F)F)c3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
11353414 64586 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 553 11 1 7 4.5 COC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181764 64586 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 553 11 1 7 4.5 COC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
11353414 64586 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 553 11 1 7 4.5 COC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181764 64586 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 553 11 1 7 4.5 COC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44347919 16341 0 None - 1 Rat 8.8 pEC50 = 8.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 606 14 3 6 4.2 C[C@H](O)CNC(=O)[C@@H](Cc1cccs1)N(C)C(=O)[C@@H](CC1=CCC(c2ccccc2)C=C1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL122939 16341 0 None - 1 Rat 8.8 pEC50 = 8.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 606 14 3 6 4.2 C[C@H](O)CNC(=O)[C@@H](Cc1cccs1)N(C)C(=O)[C@@H](CC1=CCC(c2ccccc2)C=C1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
16133832 213308 18 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/acs.jmedchem.8b01644
CHEMBL425281 213308 18 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/acs.jmedchem.8b01644
145957574 162277 0 None 57 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164328 162277 0 None 57 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
9875705 205278 1 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
CHEMBL79263 205278 1 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
156012849 177274 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4636571 177274 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156013219 177465 0 None 60 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639379 177465 0 None 60 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
11648350 88889 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3ccsc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364381 88889 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3ccsc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
59007043 88892 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2c(Cl)cccc2c1 10.6019/CHEMBL2364335
CHEMBL2364384 88892 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2c(Cl)cccc2c1 10.6019/CHEMBL2364335
69197106 88935 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(C)s3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364426 88935 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(C)s3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
24803348 88940 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 6 2 6 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1F 10.6019/CHEMBL2364335
CHEMBL2364430 88940 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 6 2 6 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1F 10.6019/CHEMBL2364335
69197228 88986 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 445 5 2 5 4.6 C[C@H]1CN(c2ccc(Cl)c(NS(=O)(=O)c3ccc(-c4ccco4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364475 88986 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 445 5 2 5 4.6 C[C@H]1CN(c2ccc(Cl)c(NS(=O)(=O)c3ccc(-c4ccco4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
16114291 191270 1 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/acs.jmedchem.1c02191
CHEMBL5190973 191270 1 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/acs.jmedchem.1c02191
16114292 96905 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm701292s
CHEMBL266063 96905 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm701292s
9875705 205278 1 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
CHEMBL79263 205278 1 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1016/j.bmc.2007.01.057
44436850 91520 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 564 11 4 6 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL240509 91520 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 564 11 4 6 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44447840 94963 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 497 14 4 10 0.9 CC(C)(N)C(=O)N[C@H](COCc1cccc(Cl)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254766 94963 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 497 14 4 10 0.9 CC(C)(N)C(=O)N[C@H](COCc1cccc(Cl)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44447854 94936 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 469 14 4 10 0.7 CC(C)(N)C(=O)N[C@H](COCC1CCCCC1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254566 94936 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 469 14 4 10 0.7 CC(C)(N)C(=O)N[C@H](COCC1CCCCC1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL105462 208445 38 None 12 2 Rat 8.8 pEC50 = 8.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm980197u
44447844 94848 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.3 CC(C)(N)C(=O)N[C@H](COCc1cccc(C(F)(F)F)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL253965 94848 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.3 CC(C)(N)C(=O)N[C@H](COCc1cccc(C(F)(F)F)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44450017 96317 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 461 15 4 9 0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL261544 96317 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 461 15 4 9 0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCO 10.1016/j.bmcl.2008.03.059
10118326 24061 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 509 9 4 4 3.7 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1ccc2ccccc2c1)C1CCNCC1 10.1016/j.bmc.2007.01.057
CHEMBL133848 24061 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 509 9 4 4 3.7 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1ccc2ccccc2c1)C1CCNCC1 10.1016/j.bmc.2007.01.057
10458218 27456 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CC(=O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
CHEMBL13687 27456 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CC(=O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
10745618 112960 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 568 13 2 4 4.5 CN(C(=O)/C=C/CC(C)(C)N)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)NCC1CC1 10.1021/jm980197u
CHEMBL331093 112960 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 568 13 2 4 4.5 CN(C(=O)/C=C/CC(C)(C)N)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)NCC1CC1 10.1021/jm980197u
10118326 24061 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 509 9 4 4 3.7 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1ccc2ccccc2c1)C1CCNCC1 10.1016/j.bmc.2007.01.057
CHEMBL133848 24061 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 509 9 4 4 3.7 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1ccc2ccccc2c1)C1CCNCC1 10.1016/j.bmc.2007.01.057
156010457 177030 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4632657 177030 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2)on1 10.1021/acs.jmedchem.0c00828
23649669 153943 9 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL398372 153943 9 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.03.059
23649669 153943 9 None - 1 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1021/jm7010595
CHEMBL398372 153943 9 None - 1 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1021/jm7010595
23649669 153943 9 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.05.100
CHEMBL398372 153943 9 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.05.100
23649669 153943 9 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL398372 153943 9 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44437955 10293 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 534 11 4 6 2.6 NCC(O)CNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCCN1C(=O)CCSc2ccccc21 10.1016/j.bmc.2007.01.057
CHEMBL1162063 10293 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 534 11 4 6 2.6 NCC(O)CNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCCN1C(=O)CCSc2ccccc21 10.1016/j.bmc.2007.01.057
10626337 101198 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1016/j.bmc.2007.01.057
CHEMBL295984 101198 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1016/j.bmc.2007.01.057
156010457 177030 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4632657 177030 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 557 7 3 7 2.3 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccc(Cl)cc2)on1 10.1021/acs.jmedchem.0c00828
156012445 177311 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637284 177311 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156015928 177557 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4640615 177557 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44452750 96228 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 481 7 2 6 4.4 COc1cccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)cc2)c1 10.1016/j.bmcl.2007.12.021
CHEMBL261030 96228 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 481 7 2 6 4.4 COc1cccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)cc2)c1 10.1016/j.bmcl.2007.12.021
44452932 97559 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 475 6 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1F 10.1016/j.bmcl.2007.12.021
CHEMBL270790 97559 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 475 6 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1F 10.1016/j.bmcl.2007.12.021
44570700 183935 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 486 6 2 6 2.1 COc1cccc(C(=O)Nc2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@H](N)C3)cc2)c1 10.1016/j.bmcl.2008.12.042
CHEMBL481620 183935 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 486 6 2 6 2.1 COc1cccc(C(=O)Nc2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@H](N)C3)cc2)c1 10.1016/j.bmcl.2008.12.042
69197169 88907 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364399 88907 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11641478 88915 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)s1 10.6019/CHEMBL2364335
CHEMBL2364407 88915 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)s1 10.6019/CHEMBL2364335
24803350 88951 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1C 10.6019/CHEMBL2364335
CHEMBL2364441 88951 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1C 10.6019/CHEMBL2364335
11547664 88991 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)c2)c(F)c1 10.6019/CHEMBL2364335
CHEMBL2364480 88991 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)c2)c(F)c1 10.6019/CHEMBL2364335
44579802 186744 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(Cc1cccc(Cl)c1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL488965 186744 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(Cc1cccc(Cl)c1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44444572 93990 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 498 5 1 7 4.1 COc1cc2c(cc1N1C[C@@H](C)NC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL248745 93990 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 498 5 1 7 4.1 COc1cc2c(cc1N1C[C@@H](C)NC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
145962494 162050 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160705 162050 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145951150 162752 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4171914 162752 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
44434120 89878 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 523 15 3 9 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCCNC(=O)OCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL237926 89878 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 523 15 3 9 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCCNC(=O)OCc1ccccc1 10.1016/j.bmcl.2007.07.099
9827234 5304 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 498 9 5 4 3.1 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1c[nH]c2ccccc12)C1CCNCC1 10.1016/j.bmc.2007.01.057
CHEMBL106841 5304 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 498 9 5 4 3.1 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1c[nH]c2ccccc12)C1CCNCC1 10.1016/j.bmc.2007.01.057
44411718 10274 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 467 7 2 5 3.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161825 10274 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 467 7 2 5 3.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
44437953 10292 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 522 9 3 6 1.5 NCCNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCN1C(=O)CCS(=O)(=O)c2ccccc21 10.1016/j.bmc.2007.01.057
CHEMBL1162062 10292 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 522 9 3 6 1.5 NCCNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCN1C(=O)CCS(=O)(=O)c2ccccc21 10.1016/j.bmc.2007.01.057
44293557 101061 0 None 1 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL294923 101061 0 None 1 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL540001 101061 0 None 1 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
127046473 139755 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 661 17 6 8 4.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798645 139755 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 661 17 6 8 4.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
156012203 177310 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 558 7 3 8 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1nnc(-c2ccc(F)cc2)s1 10.1021/acs.jmedchem.0c00828
CHEMBL4637255 177310 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 558 7 3 8 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1nnc(-c2ccc(F)cc2)s1 10.1021/acs.jmedchem.0c00828
156016696 177606 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641201 177606 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
11525404 95352 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
CHEMBL256808 95352 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
44571004 184022 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 431 5 1 5 2.6 CNC1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccc(C)o3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL482203 184022 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 431 5 1 5 2.6 CNC1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccc(C)o3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL105462 208445 38 None 12 2 Rat 8.0 pEC50 = 8 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/s0960-894x(97)10199-8
24969294 88851 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 460 5 3 6 3.1 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)c[nH]c3=O)cc2F)o1 10.6019/CHEMBL2364335
CHEMBL2364343 88851 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 460 5 3 6 3.1 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)c[nH]c3=O)cc2F)o1 10.6019/CHEMBL2364335
69194607 88866 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 466 6 2 6 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)cc1 10.6019/CHEMBL2364335
CHEMBL2364358 88866 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 466 6 2 6 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)cc1 10.6019/CHEMBL2364335
69197049 88867 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 472 6 2 7 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)s1 10.6019/CHEMBL2364335
CHEMBL2364359 88867 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 472 6 2 7 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)s1 10.6019/CHEMBL2364335
69195141 88885 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 431 5 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1csc2ccccc12 10.6019/CHEMBL2364335
CHEMBL2364377 88885 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 431 5 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1csc2ccccc12 10.6019/CHEMBL2364335
11682686 88898 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 395 4 2 4 3.8 C[C@H]1CN(c2cccc(NS(=O)(=O)c3cccc4ccccc34)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364390 88898 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 395 4 2 4 3.8 C[C@H]1CN(c2cccc(NS(=O)(=O)c3cccc4ccccc34)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69198021 88941 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc2cccc(Cl)c12 10.6019/CHEMBL2364335
CHEMBL2364431 88941 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc2cccc(Cl)c12 10.6019/CHEMBL2364335
11655608 88954 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 5 4.7 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)c(F)c3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364444 88954 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 5 4.7 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)c(F)c3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69194649 88988 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 479 5 2 5 5.2 C[C@H]1CN(c2ccc(Cl)c(NS(=O)(=O)c3ccc(-c4ccccc4F)s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364477 88988 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 479 5 2 5 5.2 C[C@H]1CN(c2ccc(Cl)c(NS(=O)(=O)c3ccc(-c4ccccc4F)s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69196750 88990 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 472 6 2 7 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)nc1 10.6019/CHEMBL2364335
CHEMBL2364479 88990 0 None - 1 Human 8.0 pEC50 = 8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 472 6 2 7 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)nc1 10.6019/CHEMBL2364335
23730339 148095 0 None - 1 Human 8.0 pEC50 = 8 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 475 10 3 10 0.4 CC1(O)CCN(C(=O)OCCn2nnnc2[C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)C1 10.1021/jm7010595
CHEMBL393531 148095 0 None - 1 Human 8.0 pEC50 = 8 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 475 10 3 10 0.4 CC1(O)CCN(C(=O)OCCn2nnnc2[C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)C1 10.1021/jm7010595
156016696 177606 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641201 177606 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145993528 167294 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 561 5 1 4 6.6 C#Cc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4294083 167294 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 561 5 1 4 6.6 C#Cc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
156012203 177310 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 558 7 3 8 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1nnc(-c2ccc(F)cc2)s1 10.1021/acs.jmedchem.0c00828
CHEMBL4637255 177310 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 558 7 3 8 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1nnc(-c2ccc(F)cc2)s1 10.1021/acs.jmedchem.0c00828
145950201 162918 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174476 162918 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
44281466 169358 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 436 8 2 4 2.9 Cc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
CHEMBL442151 169358 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 436 8 2 4 2.9 Cc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
44452806 96654 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 486 7 2 7 4.6 CC(C)Oc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
CHEMBL263916 96654 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 486 7 2 7 4.6 CC(C)Oc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
44452885 97786 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 481 8 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL271948 97786 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 481 8 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2007.12.021
11633712 159311 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 446 5 2 6 3.9 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
CHEMBL410013 159311 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 446 5 2 6 3.9 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
57390496 69026 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
CHEMBL1923628 69026 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
56926782 69028 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 472 4 3 4 3.0 CC[C@H](C)[C@@H]1NCCCCCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923631 69028 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 472 4 3 4 3.0 CC[C@H](C)[C@@H]1NCCCCCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926785 69031 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923634 69031 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926892 69033 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923636 69033 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926893 69034 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 nan
CHEMBL1923637 69034 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 nan
134131183 142443 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3890296 142443 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134133488 143211 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 600 4 4 5 4.1 CC[C@H](C)[C@@H]1NCCOc2ccc(F)cc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3896536 143211 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 600 4 4 5 4.1 CC[C@H](C)[C@@H]1NCCOc2ccc(F)cc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134134870 144367 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 534 3 4 5 2.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3905987 144367 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 534 3 4 5 2.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134132958 144636 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 536 3 3 5 2.4 C[C@H]1C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)NC[C@H]2C[C@@H]2c2ccccc2OCCN[C@H](C2CC2)C(=O)N1C nan
CHEMBL3908264 144636 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 536 3 3 5 2.4 C[C@H]1C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)NC[C@H]2C[C@@H]2c2ccccc2OCCN[C@H](C2CC2)C(=O)N1C nan
134132265 144946 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 548 3 4 6 2.2 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOCC2)NC1=O nan
CHEMBL3910661 144946 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 548 3 4 6 2.2 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOCC2)NC1=O nan
76460236 145435 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 472 4 3 4 3.0 CCC(C)C1NCCCCCCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3914338 145435 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 472 4 3 4 3.0 CCC(C)C1NCCCCCCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
134141159 146704 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 523 4 3 6 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3924192 146704 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 523 4 3 6 2.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](C)N(C)C1=O nan
134149092 148429 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 4 4 5 2.5 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O nan
CHEMBL3937924 148429 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 4 4 5 2.5 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O nan
134146570 148756 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3940653 148756 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134145820 149010 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 4 2.9 CC[C@H](C)[C@@H]1NCCc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3942642 149010 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 4 2.9 CC[C@H](C)[C@@H]1NCCc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134155024 150988 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 4 3 4 3.6 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3958451 150988 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 520 4 3 4 3.6 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134155282 151318 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3961108 151318 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134152627 151524 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 504 4 3 4 3.0 CC[C@H](C)[C@@H]1NCc2ccccc2C/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3963078 151524 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 504 4 3 4 3.0 CC[C@H](C)[C@@H]1NCc2ccccc2C/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134150696 152055 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 4 3.2 CCC(C)C1NCc2ccccc2CCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3967506 152055 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 4 3.2 CCC(C)C1NCc2ccccc2CCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
134150029 152091 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 518 4 3 4 3.3 CC[C@H](C)C1NCCCc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
CHEMBL3967783 152091 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 518 4 3 4 3.3 CC[C@H](C)C1NCCCc2ccccc2/C=C\CNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O nan
134153608 152346 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 4 3.2 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3970180 152346 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 506 4 3 4 3.2 CC[C@H](C)[C@@H]1NCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134154022 152801 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 532 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3973940 152801 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 532 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134151899 153295 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3978207 153295 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
134156625 153627 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 472 4 3 5 1.7 CC[C@H](C)[C@@H]1NCCOC/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3981072 153627 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 472 4 3 5 1.7 CC[C@H](C)[C@@H]1NCCOC/C=C\CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
16040587 179360 0 None -14 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human Ghrelin receptorAgonist activity at human Ghrelin receptor
ChEMBL 501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1 10.1021/jm801332q
CHEMBL473921 179360 0 None -14 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human Ghrelin receptorAgonist activity at human Ghrelin receptor
ChEMBL 501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1 10.1021/jm801332q
44576247 214199 0 None - 1 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.1c02191
CHEMBL506986 214199 0 None - 1 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.1c02191
44576247 214199 0 None - 1 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayInverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1016/j.bmcl.2016.04.003
CHEMBL506986 214199 0 None - 1 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayInverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1016/j.bmcl.2016.04.003
CHEMBL3578015 211743 0 None -33 2 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
CHEMBL3578018 211746 0 None -15 2 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
69198097 88872 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 452 6 2 6 3.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccnc2)cc1 10.6019/CHEMBL2364335
CHEMBL2364364 88872 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 452 6 2 6 3.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccnc2)cc1 10.6019/CHEMBL2364335
69198438 88874 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccnc2)s1 10.6019/CHEMBL2364335
CHEMBL2364366 88874 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccnc2)s1 10.6019/CHEMBL2364335
69196473 88883 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 452 5 2 6 4.3 C[C@H]1CN(c2cc(NS(=O)(=O)c3ccc(-c4cccs4)cc3)ccc2C#N)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364375 88883 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 452 5 2 6 4.3 C[C@H]1CN(c2cc(NS(=O)(=O)c3ccc(-c4cccs4)cc3)ccc2C#N)C[C@@H](C)N1 10.6019/CHEMBL2364335
69197657 88884 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 497 8 2 7 4.5 COc1ccc(Oc2cccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)c2)cc1 10.6019/CHEMBL2364335
CHEMBL2364376 88884 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 497 8 2 7 4.5 COc1ccc(Oc2cccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)c2)cc1 10.6019/CHEMBL2364335
69195983 88905 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 6 2 5 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccc3C)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364397 88905 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 6 2 5 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccc3C)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69196844 88922 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(F)cc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364414 88922 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(F)cc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11647817 88926 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 437 4 2 4 3.7 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)cc1 10.6019/CHEMBL2364335
CHEMBL2364418 88926 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 437 4 2 4 3.7 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)cc1 10.6019/CHEMBL2364335
69196864 88944 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 487 6 2 5 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(F)cc2F)cc1 10.6019/CHEMBL2364335
CHEMBL2364434 88944 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 487 6 2 5 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(F)cc2F)cc1 10.6019/CHEMBL2364335
69198407 88973 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 5 2 5 3.6 COc1cc(Br)ccc1S(=O)(=O)Nc1cc(N2C[C@H](C)N[C@H](C)C2)ccc1F 10.6019/CHEMBL2364335
CHEMBL2364463 88973 0 None - 1 Human 7.0 pEC50 = 7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 5 2 5 3.6 COc1cc(Br)ccc1S(=O)(=O)Nc1cc(N2C[C@H](C)N[C@H](C)C2)ccc1F 10.6019/CHEMBL2364335
44579958 191318 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 381 7 2 4 3.2 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
CHEMBL519171 191318 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 381 7 2 4 3.2 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
156020713 178064 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 477 6 3 7 0.7 Cc1csc(C(=O)N[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2C(=O)N[C@H]2CCCNC2)n1 10.1021/acs.jmedchem.0c00828
CHEMBL4647751 178064 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 477 6 3 7 0.7 Cc1csc(C(=O)N[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2C(=O)N[C@H]2CCCNC2)n1 10.1021/acs.jmedchem.0c00828
134139753 146011 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 5 3 5 2.5 CCCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3918783 146011 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 5 3 5 2.5 CCCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
44449923 96309 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 601 17 4 11 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1cccc(S(=O)(=O)CCO)c1 10.1016/j.bmcl.2008.03.059
CHEMBL261497 96309 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 601 17 4 11 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1cccc(S(=O)(=O)CCO)c1 10.1016/j.bmcl.2008.03.059
156020713 178064 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 477 6 3 7 0.7 Cc1csc(C(=O)N[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2C(=O)N[C@H]2CCCNC2)n1 10.1021/acs.jmedchem.0c00828
CHEMBL4647751 178064 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 477 6 3 7 0.7 Cc1csc(C(=O)N[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2C(=O)N[C@H]2CCCNC2)n1 10.1021/acs.jmedchem.0c00828
44434110 88483 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 515 13 3 9 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL235135 88483 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 515 13 3 9 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL3578018 211746 0 None -15 2 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
44450102 95742 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 511 14 4 10 0.6 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1ccccc1C(=O)NCCO 10.1016/j.bmcl.2008.03.059
CHEMBL258550 95742 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 511 14 4 10 0.6 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1ccccc1C(=O)NCCO 10.1016/j.bmcl.2008.03.059
16114290 137183 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 534 11 3 5 5.3 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL374992 137183 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 534 11 3 5 5.3 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
11664206 69024 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923626 69024 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
71453489 209345 15 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Val mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Val mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 209345 15 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Val mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Val mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
9870965 64284 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 509 9 1 5 5.3 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181092 64284 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 509 9 1 5 5.3 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44434051 89386 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccccc2)n1 10.1016/j.bmcl.2007.07.099
CHEMBL237058 89386 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccccc2)n1 10.1016/j.bmcl.2007.07.099
44434053 146833 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1cccc(NS(C)(=O)=O)c1 10.1016/j.bmcl.2007.07.099
CHEMBL392522 146833 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1cccc(NS(C)(=O)=O)c1 10.1016/j.bmcl.2007.07.099
145988557 167236 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 523 4 1 2 6.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C#CC3CC3)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4292914 167236 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 523 4 1 2 6.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C#CC3CC3)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL2170775 209340 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44434083 90002 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 420 10 2 7 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C/C=C/c1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL238155 90002 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 420 10 2 7 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C/C=C/c1ccccc1 10.1016/j.bmcl.2007.07.099
44436884 91523 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 565 11 5 7 3.1 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL240522 91523 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 565 11 5 7 3.1 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
16114098 141586 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 534 11 3 5 5.4 Cc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL385131 141586 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 534 11 3 5 5.4 Cc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
16113246 94648 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252643 94648 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
22888486 64288 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 552 9 2 6 5.5 CC(=O)Nc1cccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)c1 10.1016/j.bmcl.2005.02.040
CHEMBL181108 64288 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 552 9 2 6 5.5 CC(=O)Nc1cccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)c1 10.1016/j.bmcl.2005.02.040
71453489 209345 15 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02122
CHEMBL2170781 209345 15 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02122
156018539 177785 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1NC(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4643595 177785 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1NC(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
145949755 162910 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174302 162910 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
156013970 177216 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 624 7 3 6 3.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1ccc(-c2cc(C(F)(F)F)ccc2Cl)o1 10.1021/acs.jmedchem.0c00828
CHEMBL4635743 177216 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 624 7 3 6 3.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1ccc(-c2cc(C(F)(F)F)ccc2Cl)o1 10.1021/acs.jmedchem.0c00828
156018539 177785 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1NC(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4643595 177785 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 2 7 2.6 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1NC(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
69197178 88844 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(Cl)s2)cc1 10.6019/CHEMBL2364335
CHEMBL2364336 88844 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(Cl)s2)cc1 10.6019/CHEMBL2364335
69194396 88895 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 7 2 6 4.8 CCOc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364387 88895 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 7 2 6 4.8 CCOc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
69195258 88927 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 447 6 2 7 4.0 COc1ccc(NS(=O)(=O)c2ccc(-c3ccoc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364419 88927 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 447 6 2 7 4.0 COc1ccc(NS(=O)(=O)c2ccc(-c3ccoc3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11604627 88943 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1ccc(NS(=O)(=O)c2ccc(-c3ccoc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364433 88943 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1ccc(NS(=O)(=O)c2ccc(-c3ccoc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69197381 88961 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 486 6 2 7 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc(C)c(-c2cccc(C)n2)s1 10.6019/CHEMBL2364335
CHEMBL2364451 88961 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 486 6 2 7 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc(C)c(-c2cccc(C)n2)s1 10.6019/CHEMBL2364335
11576185 88968 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2nccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364458 88968 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2nccs2)cc1 10.6019/CHEMBL2364335
11633856 88994 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 453 6 2 7 3.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ncccn2)cc1 10.6019/CHEMBL2364335
CHEMBL2364483 88994 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 453 6 2 7 3.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ncccn2)cc1 10.6019/CHEMBL2364335
59007104 88997 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 1 6 4.8 COc1ccc(N2C[C@H](C)N(C)[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364486 88997 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 1 6 4.8 COc1ccc(N2C[C@H](C)N(C)[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2170779 209343 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44579824 184086 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1cccc(CN(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)c1 10.1016/j.bmcl.2008.07.120
CHEMBL482623 184086 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1cccc(CN(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)c1 10.1016/j.bmcl.2008.07.120
44579883 186813 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL489403 186813 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.120
44579861 194177 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1ccccc1 10.1016/j.bmcl.2008.07.120
CHEMBL528332 194177 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1ccccc1 10.1016/j.bmcl.2008.07.120
44579906 192595 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)[C@@H](C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL521612 192595 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)[C@@H](C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
145992125 166726 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 552 5 2 5 6.2 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(N)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4283504 166726 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 552 5 2 5 6.2 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(N)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
156016682 177742 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4642860 177742 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL2170776 209341 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(C(C)(C)C)cc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
16752689 188344 0 None -5 3 Rabbit 6.9 pEC50 = 6.9 Functional
Activity at ghrelin receptor in New Zealand White rabbit gastric antral smooth muscle by calcium mobilization-based FLIPR assayActivity at ghrelin receptor in New Zealand White rabbit gastric antral smooth muscle by calcium mobilization-based FLIPR assay
ChEMBL 568 10 2 4 6.6 COc1cccc(CCN(Cc2ccccc2-c2ccc(CN3C[C@H](C)N[C@H](C)C3)cc2)C(=O)NC2CCCCC2)c1 10.1016/j.bmcl.2008.10.071
CHEMBL501315 188344 0 None -5 3 Rabbit 6.9 pEC50 = 6.9 Functional
Activity at ghrelin receptor in New Zealand White rabbit gastric antral smooth muscle by calcium mobilization-based FLIPR assayActivity at ghrelin receptor in New Zealand White rabbit gastric antral smooth muscle by calcium mobilization-based FLIPR assay
ChEMBL 568 10 2 4 6.6 COc1cccc(CCN(Cc2ccccc2-c2ccc(CN3C[C@H](C)N[C@H](C)C3)cc2)C(=O)NC2CCCCC2)c1 10.1016/j.bmcl.2008.10.071
44444557 154662 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 493 4 0 5 3.7 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(S(=O)(=O)c1cccc(Br)c1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL399704 154662 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 493 4 0 5 3.7 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(S(=O)(=O)c1cccc(Br)c1)CC2 10.1016/j.bmcl.2007.09.067
145957404 162025 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)c(F)cc21 10.1021/acs.jmedchem.8b00322
CHEMBL4160261 162025 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)c(F)cc21 10.1021/acs.jmedchem.8b00322
145955250 162500 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 4 4 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCOC3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4167776 162500 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 4 4 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCOC3)cc2c1 10.1021/acs.jmedchem.8b00322
145950261 162705 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4171137 162705 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
156014569 177208 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 599 7 2 7 2.5 CC(=O)N1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
CHEMBL4635694 177208 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 599 7 2 7 2.5 CC(=O)N1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
44452776 96299 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 453 5 2 5 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL261466 96299 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 453 5 2 5 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)cc1 10.1016/j.bmcl.2007.12.021
69196695 88857 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 467 7 2 6 4.5 COc1ccc(NS(=O)(=O)c2ccc(Oc3ccccc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364349 88857 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 467 7 2 6 4.5 COc1ccc(NS(=O)(=O)c2ccc(Oc3ccccc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
59007058 88865 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 6 3.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)s1 10.6019/CHEMBL2364335
CHEMBL2364357 88865 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 6 3.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)s1 10.6019/CHEMBL2364335
156016682 177742 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4642860 177742 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44579842 184727 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccccc1Cl 10.1016/j.bmcl.2008.07.120
CHEMBL485091 184727 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccccc1Cl 10.1016/j.bmcl.2008.07.120
145986461 167189 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4291926 167189 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
145950261 162705 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4171137 162705 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
10602593 112815 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 542 12 2 4 4.1 CCNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL330860 112815 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 542 12 2 4 4.1 CCNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
44391038 64555 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 555 13 1 4 5.9 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CCCc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181627 64555 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 555 13 1 4 5.9 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CCCc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL2170783 209347 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](NC(=O)[C@@H](N)CCCCN)C(c1ccccc1)c1ccccc1)C(N)=O 10.1021/jm300414b
CHEMBL2170779 209343 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
156013970 177216 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 624 7 3 6 3.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1ccc(-c2cc(C(F)(F)F)ccc2Cl)o1 10.1021/acs.jmedchem.0c00828
CHEMBL4635743 177216 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 624 7 3 6 3.9 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1ccc(-c2cc(C(F)(F)F)ccc2Cl)o1 10.1021/acs.jmedchem.0c00828
156014569 177208 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 599 7 2 7 2.5 CC(=O)N1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
CHEMBL4635694 177208 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 599 7 2 7 2.5 CC(=O)N1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
56926173 68983 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923501 68983 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
134138625 148006 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 494 3 3 5 1.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3934561 148006 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 494 3 3 5 1.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
155526063 171012 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1174 34 16 14 -2.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4456830 171012 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1174 34 16 14 -2.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
145957404 162025 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)c(F)cc21 10.1021/acs.jmedchem.8b00322
CHEMBL4160261 162025 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)c(F)cc21 10.1021/acs.jmedchem.8b00322
145955250 162500 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 4 4 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCOC3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4167776 162500 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 4 4 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCOC3)cc2c1 10.1021/acs.jmedchem.8b00322
44454060 155308 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL403180 155308 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
57399248 69015 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at ghrelin receptor by cell based assayAgonist activity at ghrelin receptor by cell based assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm1012374
CHEMBL1923617 69015 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at ghrelin receptor by cell based assayAgonist activity at ghrelin receptor by cell based assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm1012374
145949755 162910 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174302 162910 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
44434109 146256 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 529 13 2 9 1.8 CN(c1ccccc1CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N)S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL392076 146256 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 529 13 2 9 1.8 CN(c1ccccc1CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N)S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
9890375 98242 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL274599 98242 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL558802 98242 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
44436876 146994 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 580 11 4 7 4.6 COc1ccc(N2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL392663 146994 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 580 11 4 7 4.6 COc1ccc(N2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
9890375 98242 0 None -1 3 Rat 7.9 pEC50 = 7.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/s0960-894x(97)10199-8
CHEMBL274599 98242 0 None -1 3 Rat 7.9 pEC50 = 7.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/s0960-894x(97)10199-8
CHEMBL558802 98242 0 None -1 3 Rat 7.9 pEC50 = 7.9 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/s0960-894x(97)10199-8
9890375 98242 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL274599 98242 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL558802 98242 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
44281466 169358 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 436 8 2 4 2.9 Cc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
CHEMBL442151 169358 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 436 8 2 4 2.9 Cc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
162672839 182998 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 681 14 3 7 5.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4793824 182998 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 681 14 3 7 5.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.9b02122
22888428 64320 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 508 9 2 4 4.9 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)NC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181247 64320 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 508 9 2 4 4.9 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)NC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
23730227 147849 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 477 15 4 10 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCCO 10.1021/jm7010595
CHEMBL393330 147849 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 477 15 4 10 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCCO 10.1021/jm7010595
44450133 160369 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 481 13 3 10 -0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCNC(=O)CCS(C)(=O)=O 10.1016/j.bmcl.2008.03.059
CHEMBL411122 160369 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 481 13 3 10 -0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCNC(=O)CCS(C)(=O)=O 10.1016/j.bmcl.2008.03.059
44579821 184204 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1ccccc1Cl 10.1016/j.bmcl.2008.07.120
CHEMBL483455 184204 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1ccccc1Cl 10.1016/j.bmcl.2008.07.120
44579879 186971 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)c1 10.1016/j.bmcl.2008.07.120
CHEMBL490627 186971 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)c1 10.1016/j.bmcl.2008.07.120
44450071 96556 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 489 15 3 10 0.6 CCOC(=O)CCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
CHEMBL263141 96556 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 489 15 3 10 0.6 CCOC(=O)CCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
16113906 137198 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 612 12 5 5 6.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
CHEMBL375102 137198 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 612 12 5 5 6.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
44579752 186936 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 377 8 1 4 3.7 CCC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(CC#N)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL490390 186936 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 377 8 1 4 3.7 CCC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(CC#N)cc1 10.1016/j.bmcl.2008.07.120
44436887 90930 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 563 11 5 6 3.7 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL239464 90930 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 563 11 5 6 3.7 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44434076 89748 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 513 10 2 9 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC1CN(S(C)(=O)=O)c2ccccc21 10.1016/j.bmcl.2007.07.099
CHEMBL237717 89748 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 513 10 2 9 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC1CN(S(C)(=O)=O)c2ccccc21 10.1016/j.bmcl.2007.07.099
145952740 162477 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4167481 162477 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
23648250 79134 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 585 10 4 5 6.0 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
CHEMBL2113327 79134 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 585 10 4 5 6.0 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
16113577 84907 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 573 12 4 5 5.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
CHEMBL223725 84907 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 573 12 4 5 5.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
162657465 181017 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 652 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc[nH]2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4759418 181017 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 652 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc[nH]2)cc1 10.1021/acs.jmedchem.9b02122
44444574 93991 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 484 5 1 7 3.8 COc1cc2c(cc1N1CCNC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL248746 93991 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 484 5 1 7 3.8 COc1cc2c(cc1N1CCNC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
145952740 162477 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4167481 162477 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
11532288 96891 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 441 6 2 7 2.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-n2cccn2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL265950 96891 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 441 6 2 7 2.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-n2cccn2)cc1 10.1016/j.bmcl.2007.12.021
11576186 155201 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 458 6 2 7 3.8 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccn3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.1016/j.bmcl.2007.12.021
CHEMBL402632 155201 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 458 6 2 7 3.8 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccn3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.1016/j.bmcl.2007.12.021
44570964 183857 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 407 4 1 5 1.7 Cc1ccc(-c2ccc(S(=O)(=O)N3CC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL481014 183857 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 407 4 1 5 1.7 Cc1ccc(-c2ccc(S(=O)(=O)N3CC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
44570921 183931 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 413 4 1 4 2.5 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL481601 183931 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 413 4 1 4 2.5 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
59007073 88845 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 442 6 2 7 3.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)nc1 10.6019/CHEMBL2364335
CHEMBL2364337 88845 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 442 6 2 7 3.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)nc1 10.6019/CHEMBL2364335
69197749 88854 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 425 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2ccc3ccccc3c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364346 88854 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 425 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2ccc3ccccc3c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11682796 88856 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 401 6 2 5 3.3 COc1ccc(NS(=O)(=O)/C=C/c2ccccc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364348 88856 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 401 6 2 5 3.3 COc1ccc(NS(=O)(=O)/C=C/c2ccccc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69198460 88868 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.6019/CHEMBL2364335
CHEMBL2364360 88868 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.6019/CHEMBL2364335
69198360 88876 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 466 6 2 6 4.1 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)n3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364368 88876 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 466 6 2 6 4.1 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)n3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11683967 88888 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2cccs2)c1 10.6019/CHEMBL2364335
CHEMBL2364380 88888 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2cccs2)c1 10.6019/CHEMBL2364335
69195261 88896 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 7 2 6 5.2 CC(C)Oc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364388 88896 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 7 2 6 5.2 CC(C)Oc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
11516766 88900 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 395 4 2 4 3.8 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc4ccccc4c3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364392 88900 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 395 4 2 4 3.8 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc4ccccc4c3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11525161 88957 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 447 5 2 5 4.2 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)c(F)c3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364447 88957 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 447 5 2 5 4.2 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)c(F)c3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69194533 88987 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 6 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc(F)c(-c2ccco2)cc1F 10.6019/CHEMBL2364335
CHEMBL2364476 88987 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 6 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc(F)c(-c2ccco2)cc1F 10.6019/CHEMBL2364335
69197165 88999 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 427 5 3 6 3.6 C[C@H]1CN(c2ccc(O)c(NS(=O)(=O)c3ccc(-c4ccco4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364488 88999 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 427 5 3 6 3.6 C[C@H]1CN(c2ccc(O)c(NS(=O)(=O)c3ccc(-c4ccco4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
44579777 186960 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1)C(=O)N(Cc1ccccc1Cl)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL490601 186960 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1)C(=O)N(Cc1ccccc1Cl)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44454432 155234 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
CHEMBL402808 155234 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
44434112 168836 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2cc3ccccc3n2S(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL438154 168836 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2cc3ccccc3n2S(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
44579908 186850 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 C[C@@H](Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL489610 186850 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 C[C@@H](Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
145954311 162462 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4167267 162462 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
44434124 88629 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 343 8 2 8 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CC#N)n1 10.1016/j.bmcl.2007.07.099
CHEMBL235817 88629 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 343 8 2 8 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CC#N)n1 10.1016/j.bmcl.2007.07.099
162659161 181367 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 642 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)Cc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4763471 181367 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 642 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)Cc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
44444556 94373 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 471 6 0 5 4.4 CCOc1ccc(CC(=O)N2CCc3cc(OC)c(N4C[C@H](C)N(C)[C@H](C)C4)cc32)cc1Cl 10.1016/j.bmcl.2007.09.067
CHEMBL250973 94373 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 471 6 0 5 4.4 CCOc1ccc(CC(=O)N2CCc3cc(OC)c(N4C[C@H](C)N(C)[C@H](C)C4)cc32)cc1Cl 10.1016/j.bmcl.2007.09.067
145950963 162782 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4172411 162782 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145952396 162979 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
CHEMBL4175534 162979 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
156011695 177331 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 8 2 7 2.2 O=CN1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
CHEMBL4637585 177331 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 8 2 7 2.2 O=CN1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
44452887 159554 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 451 6 2 5 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2007.12.021
CHEMBL410282 159554 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 451 6 2 5 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2007.12.021
46882522 5680 0 None -39 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 440 7 2 5 3.6 CC(C)Oc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1078208 5680 0 None -39 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 440 7 2 5 3.6 CC(C)Oc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
69195349 88879 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 453 5 2 5 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(Br)c1 10.6019/CHEMBL2364335
CHEMBL2364371 88879 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 453 5 2 5 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(Br)c1 10.6019/CHEMBL2364335
69198352 89000 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 6 2 6 4.0 COc1ccc(N2CCN[C@@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364489 89000 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 6 2 6 4.0 COc1ccc(N2CCN[C@@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
44446188 155367 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL403542 155367 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
145954311 162462 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4167267 162462 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
46882521 5679 0 None -158 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 458 6 2 4 4.5 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1078207 5679 0 None -158 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 458 6 2 4 4.5 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.09.027
44445620 154654 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 571 11 2 6 6.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccc2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL399651 154654 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 571 11 2 6 6.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccc2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
22862453 98431 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 490 5 4 5 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CC(O)c1ccccc1O2 10.1016/s0960-894x(97)10199-8
CHEMBL275795 98431 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 490 5 4 5 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CC(O)c1ccccc1O2 10.1016/s0960-894x(97)10199-8
10675061 96514 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 598 13 2 5 4.3 CN(C(=O)/C=C/CC(C)(C)N)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)NCC1CCCO1 10.1021/jm980197u
CHEMBL262889 96514 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 598 13 2 5 4.3 CN(C(=O)/C=C/CC(C)(C)N)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)NCC1CCCO1 10.1021/jm980197u
10026738 162745 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL417182 162745 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL557206 162745 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
56926464 69010 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)N(C)C1=O nan
CHEMBL1923612 69010 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)N(C)C1=O nan
155540883 172933 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.36 +/- 0.01 nM)Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.36 +/- 0.01 nM)
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4517399 172933 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.36 +/- 0.01 nM)Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.36 +/- 0.01 nM)
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
10210658 10294 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 593 13 5 5 3.6 NCCCCNC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1 10.1016/j.bmc.2007.01.057
CHEMBL1162064 10294 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 593 13 5 5 3.6 NCCCCNC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1 10.1016/j.bmc.2007.01.057
145952396 162979 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
CHEMBL4175534 162979 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
CHEMBL2170784 209348 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
134139080 147658 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 4 4 5 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
CHEMBL3931856 147658 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 4 4 5 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
156011695 177331 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 8 2 7 2.2 O=CN1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
CHEMBL4637585 177331 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 8 2 7 2.2 O=CN1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1 10.1021/acs.jmedchem.0c00828
CHEMBL2170697 209334 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44434080 89882 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2007.07.099
44434080 89882 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL237933 89882 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL237933 89882 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2008.01.100
10210658 10294 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 593 13 5 5 3.6 NCCCCNC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1 10.1016/j.bmc.2007.01.057
CHEMBL1162064 10294 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 593 13 5 5 3.6 NCCCCNC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1 10.1016/j.bmc.2007.01.057
10026738 162745 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL417182 162745 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL557206 162745 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
10530983 168361 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 564 11 2 4 4.0 CNC(=O)[C@@H](Cc1ccc(F)c(F)c1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL434609 168361 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 564 11 2 4 4.0 CNC(=O)[C@@H](Cc1ccc(F)c(F)c1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
44391003 123295 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 531 10 1 4 5.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)c1ccccc1F)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL361612 123295 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 531 10 1 4 5.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)c1ccccc1F)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL2170780 209344 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
145950963 162782 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4172411 162782 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
127047409 139606 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 888 24 8 10 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C(CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797639 139606 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 888 24 8 10 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C(CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
10745533 140095 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL380096 140095 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
44437971 202497 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 7 2 4 3.9 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
CHEMBL611489 202497 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 7 2 4 3.9 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
16113693 137991 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 589 12 4 6 5.6 COc1cccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL376471 137991 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 589 12 4 6 5.6 COc1cccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
11692516 69019 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 554 3 3 5 3.1 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923621 69019 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 554 3 3 5 3.1 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
155557019 174563 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.34 +/- 0.12 nM)Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.34 +/- 0.12 nM)
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4556887 174563 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.34 +/- 0.12 nM)Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.34 +/- 0.12 nM)
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
9810101 99221 17 None -5 2 Rat 7.8 pEC50 = 7.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL281764 99221 17 None -5 2 Rat 7.8 pEC50 = 7.8 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
10745533 140095 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL380096 140095 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
44437971 202497 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 7 2 4 3.9 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
CHEMBL611489 202497 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 7 2 4 3.9 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
44579909 186879 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL489819 186879 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
44436882 145991 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 524 10 4 6 4.2 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1Cc1ccco1)C1CCNCC1 10.1021/jm0704550
CHEMBL391859 145991 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 524 10 4 6 4.2 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1Cc1ccco1)C1CCNCC1 10.1021/jm0704550
CHEMBL2170698 209335 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44434122 89482 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 385 11 2 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCCCC#N)n1 10.1016/j.bmcl.2007.07.099
CHEMBL237302 89482 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 385 11 2 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCCCC#N)n1 10.1016/j.bmcl.2007.07.099
145992142 166747 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 475 4 2 3 5.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(O)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4283858 166747 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 475 4 2 3 5.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(O)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL3578006 211737 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)O 10.1021/jm501702q
145953016 162563 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
CHEMBL4168863 162563 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
44454304 97575 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
CHEMBL270876 97575 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
44454092 97621 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
CHEMBL271082 97621 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
44454338 97807 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL272085 97807 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
22867310 30010 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 474 5 4 4 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)Cc1ccccc1C2O 10.1016/s0960-894x(97)10199-8
CHEMBL13891 30010 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 474 5 4 4 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)Cc1ccccc1C2O 10.1016/s0960-894x(97)10199-8
162653802 180507 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 656 15 4 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CCc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4753592 180507 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 656 15 4 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CCc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
44436886 161931 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 595 12 5 8 3.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL415674 161931 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 595 12 5 8 3.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
9987037 12000 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1183385 12000 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL294324 12000 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
44391008 64837 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 481 9 1 5 4.6 CCN(CC)CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL182137 64837 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 481 9 1 5 4.6 CCN(CC)CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
22888379 168289 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 584 12 2 5 4.8 CC(=O)NC(C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C)c1ccccc1 10.1016/j.bmcl.2005.02.040
CHEMBL434152 168289 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 584 12 2 5 4.8 CC(=O)NC(C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C)c1ccccc1 10.1016/j.bmcl.2005.02.040
44444564 94443 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 478 5 1 6 3.7 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1cccc(-c3ccccn3)c1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL251366 94443 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 478 5 1 6 3.7 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1cccc(-c3ccccn3)c1)CC2 10.1016/j.bmcl.2007.09.067
145961213 162139 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 3 4 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@H]3COCCN(C)C3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4162174 162139 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 3 4 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@H]3COCCN(C)C3)cc2c1 10.1021/acs.jmedchem.8b00322
145953016 162563 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
CHEMBL4168863 162563 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
145949595 162700 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4171040 162700 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145974293 163000 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4175823 163000 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
44452929 97515 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2ccco2)c1 10.1016/j.bmcl.2007.12.021
CHEMBL270573 97515 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2ccco2)c1 10.1016/j.bmcl.2007.12.021
46882396 5812 0 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 452 8 2 4 4.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cnc(C)[nH]2)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1079187 5812 0 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 452 8 2 4 4.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cnc(C)[nH]2)CC3)cc1 10.1016/j.bmcl.2009.09.027
44570698 183934 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 456 5 2 5 2.0 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(NC(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL481619 183934 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 456 5 2 5 2.0 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(NC(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
24969292 88848 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 444 5 2 6 3.8 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccn3)cc2F)o1 10.6019/CHEMBL2364335
CHEMBL2364340 88848 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 444 5 2 6 3.8 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccn3)cc2F)o1 10.6019/CHEMBL2364335
69194665 88881 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 476 6 2 7 3.9 COc1cc(F)c(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.6019/CHEMBL2364335
CHEMBL2364373 88881 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 476 6 2 7 3.9 COc1cc(F)c(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.6019/CHEMBL2364335
11524465 88901 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 413 4 2 4 4.0 C[C@H]1CN(c2cccc(NS(=O)(=O)c3cccc(Cl)c3Cl)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364393 88901 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 413 4 2 4 4.0 C[C@H]1CN(c2cccc(NS(=O)(=O)c3cccc(Cl)c3Cl)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11576404 88912 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 469 6 2 5 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364404 88912 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 469 6 2 5 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69194865 88931 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 409 4 2 4 4.1 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc2ccccc12 10.6019/CHEMBL2364335
CHEMBL2364422 88931 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 409 4 2 4 4.1 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc2ccccc12 10.6019/CHEMBL2364335
11712498 88945 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 469 6 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2F)cc1 10.6019/CHEMBL2364335
CHEMBL2364435 88945 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 469 6 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2F)cc1 10.6019/CHEMBL2364335
69195296 88950 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 5 4.7 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)cc3F)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364440 88950 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 5 4.7 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)cc3F)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11518242 88953 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.9 Cc1cc(-c2cccs2)ccc1S(=O)(=O)Nc1cc(N2C[C@H](C)N[C@H](C)C2)ccc1F 10.6019/CHEMBL2364335
CHEMBL2364443 88953 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.9 Cc1cc(-c2cccs2)ccc1S(=O)(=O)Nc1cc(N2C[C@H](C)N[C@H](C)C2)ccc1F 10.6019/CHEMBL2364335
69197366 88958 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 5 4.7 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)cc3Cl)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364448 88958 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 5 4.7 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)cc3Cl)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11503413 88975 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 454 6 2 6 3.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccn2C)cc1 10.6019/CHEMBL2364335
CHEMBL2364465 88975 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 454 6 2 6 3.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccn2C)cc1 10.6019/CHEMBL2364335
11647900 88981 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1cc(-c2ccco2)ccc1S(=O)(=O)Nc1cccc(N2C[C@H](C)N[C@H](C)C2)c1 10.6019/CHEMBL2364335
CHEMBL2364470 88981 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1cc(-c2ccco2)ccc1S(=O)(=O)Nc1cccc(N2C[C@H](C)N[C@H](C)C2)c1 10.6019/CHEMBL2364335
11669734 88982 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1cc(-c2cccs2)ccc1S(=O)(=O)Nc1cccc(N2C[C@H](C)N[C@H](C)C2)c1 10.6019/CHEMBL2364335
CHEMBL2364471 88982 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1cc(-c2cccs2)ccc1S(=O)(=O)Nc1cccc(N2C[C@H](C)N[C@H](C)C2)c1 10.6019/CHEMBL2364335
44391007 64836 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 480 9 1 4 4.1 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)N(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL182136 64836 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 480 9 1 4 4.1 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)N(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
145994050 167321 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 615 6 1 6 7.1 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4294493 167321 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 615 6 1 6 7.1 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
156016392 177622 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641386 177622 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL3578006 211737 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)O 10.1021/jm501702q
25098836 191434 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL519322 191434 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
145957574 162277 0 None 57 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164328 162277 0 None 57 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
44411745 10276 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161827 10276 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
10626337 101198 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1016/j.bmc.2007.01.057
CHEMBL295984 101198 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1016/j.bmc.2007.01.057
156013219 177465 0 None 60 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639379 177465 0 None 60 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
22888352 63907 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 537 11 1 6 4.9 CC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180659 63907 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 537 11 1 6 4.9 CC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
22888352 63907 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 537 11 1 6 4.9 CC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180659 63907 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
ChEMBL 537 11 1 6 4.9 CC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
10649999 17074 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 534 11 2 5 3.8 CNC(=O)[C@@H](Cc1cccs1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL125498 17074 0 None - 1 Rat 8.7 pEC50 = 8.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 534 11 2 5 3.8 CNC(=O)[C@@H](Cc1cccs1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
156015928 177557 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4640615 177557 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156012445 177311 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637284 177311 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44411634 10273 1 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161824 10273 1 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
44411634 10273 1 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161824 10273 1 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
44390986 64639 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 1 5 5.2 COc1ccccc1CC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181832 64639 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 1 5 5.2 COc1ccccc1CC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL2170695 209332 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1csc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
156011766 177284 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 569 6 2 7 2.2 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N1C[C@H]2CCNC[C@H]21)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4636780 177284 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 569 6 2 7 2.2 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N1C[C@H]2CCNC[C@H]21)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
44281449 113367 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 559 12 4 7 1.4 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)CC(=O)O)CC1 10.1016/j.bmc.2007.01.057
CHEMBL33182 113367 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 559 12 4 7 1.4 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)CC(=O)O)CC1 10.1016/j.bmc.2007.01.057
44281449 113367 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 559 12 4 7 1.4 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)CC(=O)O)CC1 10.1016/j.bmc.2007.01.057
CHEMBL33182 113367 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 559 12 4 7 1.4 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)CC(=O)O)CC1 10.1016/j.bmc.2007.01.057
23648249 79133 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 557 9 4 5 5.4 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1)C1CCNCC1 10.1021/jm0704550
CHEMBL2113326 79133 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 557 9 4 5 5.4 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1)C1CCNCC1 10.1021/jm0704550
10166594 64606 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 563 8 1 5 6.6 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccc(C(F)(F)F)cc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181786 64606 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 563 8 1 5 6.6 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccc(C(F)(F)F)cc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44391010 64844 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 541 9 1 6 6.3 CSc1ccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
CHEMBL182158 64844 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 541 9 1 6 6.3 CSc1ccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
23648244 91985 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
CHEMBL241775 91985 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
155557019 174563 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.40 +/- 0.05 nM)Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.40 +/- 0.05 nM)
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4556887 174563 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.40 +/- 0.05 nM)Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.40 +/- 0.05 nM)
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
44444565 94471 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 474 5 1 8 3.4 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccon3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL251573 94471 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 474 5 1 8 3.4 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccon3)s1)CC2 10.1016/j.bmcl.2007.09.067
145957075 162255 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164040 162255 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
44411745 10276 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161827 10276 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
156013684 177241 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccc(Cl)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4636178 177241 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccc(Cl)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
156011766 177284 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 569 6 2 7 2.2 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N1C[C@H]2CCNC[C@H]21)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4636780 177284 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 569 6 2 7 2.2 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N1C[C@H]2CCNC[C@H]21)c1cc(-c2ccccc2Cl)on1 10.1021/acs.jmedchem.0c00828
11539642 97900 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 448 6 2 8 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnco2)s1 10.1016/j.bmcl.2007.12.021
CHEMBL272540 97900 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 448 6 2 8 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnco2)s1 10.1016/j.bmcl.2007.12.021
44570702 183812 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 463 4 1 5 3.1 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3C[C@H](C)N[C@H](C)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL480639 183812 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 463 4 1 5 3.1 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3C[C@H](C)N[C@H](C)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
11683968 88887 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3ccsc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364379 88887 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3ccsc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69197883 88910 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2F)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364402 88910 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2F)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69195597 88923 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2Cl)s1 10.6019/CHEMBL2364335
CHEMBL2364415 88923 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2Cl)s1 10.6019/CHEMBL2364335
59007081 88937 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 5 5.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(Cl)c2)cc1 10.6019/CHEMBL2364335
CHEMBL2364428 88937 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 5 5.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(Cl)c2)cc1 10.6019/CHEMBL2364335
11648834 88992 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)c2)cc1F 10.6019/CHEMBL2364335
CHEMBL2364481 88992 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)c2)cc1F 10.6019/CHEMBL2364335
44411753 10278 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161829 10278 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
44411753 10278 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161829 10278 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
10415000 168043 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 11 3 6 2.7 CC(C)S(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
CHEMBL432461 168043 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 11 3 6 2.7 CC(C)S(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
71453489 209345 15 None - 1 Human 8.6 pEC50 = 8.6 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Phe119:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Phe119:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 209345 15 None - 1 Human 8.6 pEC50 = 8.6 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Phe119:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Phe119:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
156013684 177241 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccc(Cl)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4636178 177241 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 571 7 3 7 2.6 Cc1oc(-c2ccc(Cl)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
10415000 168043 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 11 3 6 2.7 CC(C)S(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
CHEMBL432461 168043 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 543 11 3 6 2.7 CC(C)S(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
156019457 177918 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645625 177918 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44449922 96192 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 615 17 3 11 1.0 CN(CCc1cccc(S(=O)(=O)CCO)c1)C(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
CHEMBL260849 96192 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 615 17 3 11 1.0 CN(CCc1cccc(S(=O)(=O)CCO)c1)C(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
44269019 98198 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 474 5 3 4 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CCc3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
CHEMBL274340 98198 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 474 5 3 4 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CCc3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
44579840 184725 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1cccc(Cl)c1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL485090 184725 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1cccc(Cl)c1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44579907 187024 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)[C@H](C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL491044 187024 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)[C@H](C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
44579805 187042 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1Cl)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL491221 187042 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1Cl)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44434113 88620 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 452 10 2 9 1.5 COC(=O)C(c1ccccc1)n1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL235793 88620 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 452 10 2 9 1.5 COC(=O)C(c1ccccc1)n1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
127048060 139836 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 789 20 6 10 5.4 COC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799222 139836 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 789 20 6 10 5.4 COC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
57399248 69015 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923617 69015 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
44268965 24030 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 472 5 3 4 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(Cc3ccccc3C2=O)C1 10.1016/s0960-894x(97)10199-8
CHEMBL13383 24030 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 472 5 3 4 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(Cc3ccccc3C2=O)C1 10.1016/s0960-894x(97)10199-8
10675800 113767 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 654 11 2 4 4.3 CNC(=O)[C@@H](Cc1ccc(I)cc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL332414 113767 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 654 11 2 4 4.3 CNC(=O)[C@@H](Cc1ccc(I)cc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
44391002 123884 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 507 10 1 4 5.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL362798 123884 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 507 10 1 4 5.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44579857 186900 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL490009 186900 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2Cl)c1 10.1016/j.bmcl.2008.07.120
44434018 88463 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 399 8 3 8 0.9 COC(=O)CCn1nnnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL235012 88463 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 399 8 3 8 0.9 COC(=O)CCn1nnnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
44579641 186873 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 370 7 1 4 4.0 CSc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
CHEMBL489794 186873 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 370 7 1 4 4.0 CSc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
44579996 187112 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 367 7 2 4 2.8 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)COc2ccccc2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL491835 187112 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 367 7 2 4 2.8 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)COc2ccccc2)cc1 10.1016/j.bmcl.2008.07.120
44579919 191325 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 444 9 1 4 5.3 CCC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1cccc(-c2ccccc2)c1OC 10.1016/j.bmcl.2008.07.120
CHEMBL519196 191325 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 444 9 1 4 5.3 CCC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1cccc(-c2ccccc2)c1OC 10.1016/j.bmcl.2008.07.120
44454092 97621 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
CHEMBL271082 97621 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
44450070 158627 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 461 14 4 9 0.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCC(=O)O 10.1016/j.bmcl.2008.03.059
CHEMBL409258 158627 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 461 14 4 9 0.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCC(=O)O 10.1016/j.bmcl.2008.03.059
156016392 177622 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641386 177622 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145961213 162139 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 3 4 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@H]3COCCN(C)C3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4162174 162139 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 3 4 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@H]3COCCN(C)C3)cc2c1 10.1021/acs.jmedchem.8b00322
145949595 162700 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4171040 162700 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145974293 163000 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4175823 163000 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
44390905 64427 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 544 10 1 6 3.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)S(=O)(=O)N(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181337 64427 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 544 10 1 6 3.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)S(=O)(=O)N(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44391040 64431 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 577 10 1 6 5.0 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)S(=O)(=O)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181352 64431 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 577 10 1 6 5.0 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)S(=O)(=O)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
10579444 114216 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 598 13 2 5 4.3 CN(C(=O)/C=C/CC(C)(C)N)[C@H](Cc1cccc2ccccc12)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)NCC1CCCO1 10.1021/jm980197u
CHEMBL332987 114216 0 None - 1 Rat 7.7 pEC50 = 7.7 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 598 13 2 5 4.3 CN(C(=O)/C=C/CC(C)(C)N)[C@H](Cc1cccc2ccccc12)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)NCC1CCCO1 10.1021/jm980197u
162645413 179702 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 677 14 3 7 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4744051 179702 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 677 14 3 7 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(C)cc2)cc1 10.1021/acs.jmedchem.9b02122
44293091 188162 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL49884 188162 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
16114011 138113 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 563 10 4 5 5.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(F)cc1 10.1021/jm070024h
CHEMBL376736 138113 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 563 10 4 5 5.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(F)cc1 10.1021/jm070024h
145981343 166685 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 669 6 1 6 7.6 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@H](c3ccc(-c4cnccn4)c(Cl)c3Cl)C(F)(F)F)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4282719 166685 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 669 6 1 6 7.6 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@H](c3ccc(-c4cnccn4)c(Cl)c3Cl)C(F)(F)F)CC2)ncn1 10.1021/acs.jmedchem.8b00794
44391048 62918 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 467 8 2 5 4.2 CC(C)NCCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL178502 62918 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 467 8 2 5 4.2 CC(C)NCCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
44454399 155115 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC(C#N)Cc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL402086 155115 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC(C#N)Cc1ccccc1 10.1016/j.bmcl.2008.01.100
44293091 188162 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
CHEMBL49884 188162 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1016/j.bmc.2007.01.057
155540883 172933 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4517399 172933 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
44579801 187137 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1)C(=O)N(Cc1ccc(Cl)cc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL492028 187137 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1)C(=O)N(Cc1ccc(Cl)cc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
168276220 190397 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 261 6 1 1 4.2 CCCCCCCc1cc(=O)c2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.1c02191
CHEMBL5177954 190397 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 261 6 1 1 4.2 CCCCCCCc1cc(=O)c2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.1c02191
145958774 162242 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163811 162242 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145950877 162971 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4175360 162971 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
44450135 158679 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 493 14 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1ccccc1 10.1016/j.bmcl.2008.03.059
CHEMBL409327 158679 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 493 14 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1ccccc1 10.1016/j.bmcl.2008.03.059
44454302 159356 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
CHEMBL410060 159356 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
16203237 96922 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 496 10 3 6 4.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccco1 10.1021/jm070024h
CHEMBL266199 96922 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 496 10 3 6 4.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccco1 10.1021/jm070024h
56926462 69008 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923610 69008 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
162660604 181195 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 700 15 3 9 5.0 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCN3CCCCC3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4761319 181195 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 700 15 3 9 5.0 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCN3CCCCC3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
145956753 162133 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4162000 162133 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
71453489 209345 15 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 209345 15 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44446190 94527 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL251855 94527 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
44446189 155350 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL403426 155350 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
10744738 16172 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1cccc2ccccc12)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL122420 16172 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1cccc2ccccc12)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL2170699 209336 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44454432 155234 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
CHEMBL402808 155234 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
44454397 155500 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CC(C#N)Cc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
CHEMBL404227 155500 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CC(C#N)Cc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
145949381 162691 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4170865 162691 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
22862431 30454 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 474 5 3 4 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc3O2)CC1 10.1016/s0960-894x(97)10199-8
CHEMBL13930 30454 0 None - 1 Rat 7.6 pEC50 = 7.6 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 474 5 3 4 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc3O2)CC1 10.1016/s0960-894x(97)10199-8
162653781 180458 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 732 15 4 8 6.2 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3c[nH]c4ccccc34)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4753046 180458 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 732 15 4 8 6.2 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3c[nH]c4ccccc34)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
156013764 177247 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 7 1 7 3.0 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1N(C)C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4636229 177247 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 7 1 7 3.0 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1N(C)C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
145958317 162289 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164531 162289 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145949381 162691 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4170865 162691 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
145950877 162971 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4175360 162971 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
156013764 177247 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 7 1 7 3.0 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1N(C)C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4636229 177247 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 585 7 1 7 3.0 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1N(C)C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
156020452 178010 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 4 5 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@]3(C)C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4646979 178010 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 4 5 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@]3(C)C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
24969201 88852 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 476 6 2 7 4.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)nc1NS(=O)(=O)c1ccc(-c2ccoc2)cc1Cl 10.6019/CHEMBL2364335
CHEMBL2364344 88852 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 476 6 2 7 4.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)nc1NS(=O)(=O)c1ccc(-c2ccoc2)cc1Cl 10.6019/CHEMBL2364335
69197403 88877 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 5 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc2cc(Cl)ccc2s1 10.6019/CHEMBL2364335
CHEMBL2364369 88877 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 5 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc2cc(Cl)ccc2s1 10.6019/CHEMBL2364335
59007071 88891 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 444 5 3 7 3.5 C[C@H]1CN(c2ccc(O)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364383 88891 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 444 5 3 7 3.5 C[C@H]1CN(c2ccc(O)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11547135 88904 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 461 5 2 5 5.1 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-c4ccc(Cl)s4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364396 88904 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 461 5 2 5 5.1 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-c4ccc(Cl)s4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11567764 88908 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 411 5 2 6 2.9 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-n4cccn4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364400 88908 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 411 5 2 6 2.9 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-n4cccn4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11511157 88918 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2C)s1 10.6019/CHEMBL2364335
CHEMBL2364410 88918 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2C)s1 10.6019/CHEMBL2364335
11547599 88920 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 6 5.0 COc1ccc(NS(=O)(=O)c2ccc(-c3c(C)cccc3C)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364412 88920 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 6 5.0 COc1ccc(NS(=O)(=O)c2ccc(-c3c(C)cccc3C)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69197133 88930 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)s1 10.6019/CHEMBL2364335
CHEMBL2364421 88930 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 477 6 2 7 4.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)s1 10.6019/CHEMBL2364335
69197849 88955 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 429 5 2 5 4.1 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364445 88955 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 429 5 2 5 4.1 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69198350 88962 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 6 2 9 3.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csnn2)s1 10.6019/CHEMBL2364335
CHEMBL2364452 88962 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 6 2 9 3.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csnn2)s1 10.6019/CHEMBL2364335
156020452 178010 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 4 5 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@]3(C)C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4646979 178010 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 6 4 5 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@]3(C)C(=O)N[C@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
44579860 188877 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(C[C@H]1CCCN1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL507551 188877 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(C[C@H]1CCCN1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
145956415 162039 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160541 162039 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145956415 162039 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160541 162039 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145956753 162133 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4162000 162133 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145958774 162242 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163811 162242 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145955718 162511 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4167965 162511 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145952404 162712 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4171300 162712 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL3578014 211742 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
44436816 91776 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 524 12 4 6 3.9 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CCN)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL241242 91776 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 524 12 4 6 3.9 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CCN)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44391028 64268 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 451 9 1 4 3.9 CC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181051 64268 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 451 9 1 4 3.9 CC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44390906 132077 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 467 7 2 5 4.2 CC(C)(CN)CNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL369571 132077 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 467 7 2 5 4.2 CC(C)(CN)CNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
44434052 89387 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccc(NS(C)(=O)=O)cc1 10.1016/j.bmcl.2007.07.099
CHEMBL237059 89387 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccc(NS(C)(=O)=O)cc1 10.1016/j.bmcl.2007.07.099
44450169 159726 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 471 12 3 8 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCC(F)(F)F 10.1016/j.bmcl.2008.03.059
CHEMBL410499 159726 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 471 12 3 8 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCC(F)(F)F 10.1016/j.bmcl.2008.03.059
56926894 69035 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923638 69035 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
44391027 128777 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 541 12 1 4 5.6 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CCc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL366916 128777 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 541 12 1 4 5.6 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CCc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
44579803 186745 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(Cc1ccccc1Cl)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL488966 186745 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(Cc1ccccc1Cl)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
145952404 162712 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4171300 162712 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL3578014 211742 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
11526696 71573 17 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm1012374
CHEMBL1923502 71573 17 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm1012374
CHEMBL1963249 71573 17 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm1012374
44450045 159213 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 447 14 4 9 0.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL409894 159213 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 447 14 4 9 0.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCO 10.1016/j.bmcl.2008.03.059
44434012 89045 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 479 13 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL236513 89045 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 479 13 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCc1ccccc1 10.1016/j.bmcl.2007.07.099
44454398 97570 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(C#N)c1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL270851 97570 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(C#N)c1ccccc1 10.1016/j.bmcl.2008.01.100
11526745 69039 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923642 69039 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
44391020 63834 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 543 11 1 5 5.7 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OCc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180337 63834 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 543 11 1 5 5.7 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OCc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
162643920 181756 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 679 14 4 8 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4777792 181756 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 679 14 4 8 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
155540883 172933 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.41 +/- 0.13 nM)Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.41 +/- 0.13 nM)
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4517399 172933 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.41 +/- 0.13 nM)Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.41 +/- 0.13 nM)
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
145955718 162511 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4167965 162511 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 432 4 2 5 2.0 CN1CCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
23648236 79123 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 524 13 3 7 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NCCN)c(OC)c1 10.1021/jm0704550
CHEMBL2113317 79123 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 524 13 3 7 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NCCN)c(OC)c1 10.1021/jm0704550
145958317 162289 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164531 162289 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
162649014 179917 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 702 14 4 7 6.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2c[nH]c3ccccc23)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4746362 179917 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 702 14 4 7 6.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2c[nH]c3ccccc23)cc1 10.1021/acs.jmedchem.9b02122
44434123 145525 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 343 8 2 8 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC#N 10.1016/j.bmcl.2007.07.099
CHEMBL391510 145525 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 343 8 2 8 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC#N 10.1016/j.bmcl.2007.07.099
11526696 71573 17 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923502 71573 17 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1963249 71573 17 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
122178179 121237 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1002 29 10 9 3.8 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
CHEMBL3578008 121237 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1002 29 10 9 3.8 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
145980382 166619 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4281310 166619 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
71453489 209345 15 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 209345 15 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
134149793 148581 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 5 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(CC)C1=O nan
CHEMBL3939196 148581 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
ChEMBL 508 5 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(CC)C1=O nan
145980333 166557 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 577 6 1 4 7.5 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4280040 166557 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 577 6 1 4 7.5 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
44579823 184057 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL482420 184057 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
145957075 162255 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164040 162255 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
145951150 162752 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4171914 162752 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
44449864 158806 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 539 16 4 10 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1cccc(C(=O)NCCCCO)c1 10.1016/j.bmcl.2008.03.059
CHEMBL409462 158806 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 539 16 4 10 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1cccc(C(=O)NCCCCO)c1 10.1016/j.bmcl.2008.03.059
10005618 10291 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 11 1 3 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1 10.1016/j.bmc.2007.01.057
CHEMBL1162058 10291 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 11 1 3 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1 10.1016/j.bmc.2007.01.057
15481181 77715 2 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
CHEMBL209020 77715 2 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
9810101 99221 17 None 5 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL281764 99221 17 None 5 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
15481188 141185 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1016/j.bmc.2007.01.057
CHEMBL382844 141185 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1016/j.bmc.2007.01.057
CHEMBL130229 208664 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL None None None CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1016/j.bmc.2007.01.057
16114292 96905 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
CHEMBL266063 96905 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
16114292 96905 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL266063 96905 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
23730225 154152 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 435 12 4 10 -0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCO 10.1021/jm7010595
CHEMBL398570 154152 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 435 12 4 10 -0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCO 10.1021/jm7010595
10530781 15546 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 554 12 2 4 4.2 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL122108 15546 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 554 12 2 4 4.2 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
10005618 10291 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 11 1 3 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1 10.1016/j.bmc.2007.01.057
CHEMBL1162058 10291 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 485 11 1 3 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1 10.1016/j.bmc.2007.01.057
15481181 77715 2 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
CHEMBL209020 77715 2 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
9810101 99221 17 None 5 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL281764 99221 17 None 5 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
15481188 141185 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1016/j.bmc.2007.01.057
CHEMBL382844 141185 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1016/j.bmc.2007.01.057
CHEMBL130229 208664 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL None None None CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1016/j.bmc.2007.01.057
156011385 177354 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 518 8 3 5 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCCCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637916 177354 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 518 8 3 5 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCCCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44449956 96586 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 523 14 3 9 2.0 CN(CCc1cccc(O)c1)C(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
CHEMBL263389 96586 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 523 14 3 9 2.0 CN(CCc1cccc(O)c1)C(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
44447846 94870 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 547 15 4 11 1.2 CC(C)(N)C(=O)N[C@H](COCc1cccc(OC(F)(F)F)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254166 94870 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 547 15 4 11 1.2 CC(C)(N)C(=O)N[C@H](COCc1cccc(OC(F)(F)F)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44444566 154743 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 470 5 1 7 3.4 COc1cc2c(cc1N1CCN[C@@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL400124 154743 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 470 5 1 7 3.4 COc1cc2c(cc1N1CCN[C@@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
156011385 177354 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 518 8 3 5 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCCCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637916 177354 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 518 8 3 5 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCCCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156019457 177918 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645625 177918 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44570961 192537 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 421 4 1 5 2.2 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccco3)c(F)c2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL521246 192537 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 421 4 1 5 2.2 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccco3)c(F)c2)C1 10.1016/j.bmcl.2008.12.042
69195095 88934 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)c(F)c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364425 88934 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)c(F)c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69194503 88970 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)cc1Cl 10.6019/CHEMBL2364335
CHEMBL2364460 88970 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)cc1Cl 10.6019/CHEMBL2364335
59007103 88996 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 456 6 2 7 3.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cn1 10.6019/CHEMBL2364335
CHEMBL2364485 88996 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 456 6 2 7 3.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cn1 10.6019/CHEMBL2364335
69197358 89002 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 3 6 4.1 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3O)cc2F)o1 10.6019/CHEMBL2364335
CHEMBL2364491 89002 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 3 6 4.1 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3O)cc2F)o1 10.6019/CHEMBL2364335
44450046 95827 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 501 14 4 9 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCN1CCNC1=O 10.1016/j.bmcl.2008.03.059
CHEMBL259016 95827 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 501 14 4 9 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCN1CCNC1=O 10.1016/j.bmcl.2008.03.059
23730341 89713 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 502 11 3 10 0.1 CC(=O)N[C@@H]1CCN(C(=O)OCCn2nnnc2[C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)C1 10.1021/jm7010595
CHEMBL237701 89713 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 502 11 3 10 0.1 CC(=O)N[C@@H]1CCN(C(=O)OCCn2nnnc2[C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)C1 10.1021/jm7010595
71453489 209345 15 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Asp mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Asp mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 209345 15 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Asp mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Asp mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44390914 63608 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 11 1 5 4.9 CCCOC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180093 63608 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 11 1 5 4.9 CCCOC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
22888424 122972 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 541 11 1 4 5.7 CC(C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C)c1ccccc1 10.1016/j.bmcl.2005.02.040
CHEMBL360877 122972 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 541 11 1 4 5.7 CC(C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C)c1ccccc1 10.1016/j.bmcl.2005.02.040
71453489 209345 15 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 209345 15 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
162671996 182807 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 707 16 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)NCCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4791255 182807 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 707 16 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)NCCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
23730228 89563 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 477 14 3 10 0.6 CN(CCCCO)C(=O)OCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1021/jm7010595
CHEMBL237492 89563 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 477 14 3 10 0.6 CN(CCCCO)C(=O)OCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1021/jm7010595
71453489 209345 15 None - 1 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 209345 15 None - 1 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44444568 93949 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 470 5 1 7 3.4 COc1cc2c(cc1N1CCN[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL248542 93949 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 470 5 1 7 3.4 COc1cc2c(cc1N1CCN[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
15481185 77232 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
CHEMBL207970 77232 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
156011736 177399 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 605 7 3 7 3.0 Cc1oc(-c2ccc(C(F)(F)F)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4638566 177399 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 605 7 3 7 3.0 Cc1oc(-c2ccc(C(F)(F)F)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
25022506 95238 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 457 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL256263 95238 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 457 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2007.12.021
24803347 155004 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL401548 155004 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1 10.1016/j.bmcl.2007.12.021
46882394 5810 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 438 8 2 4 4.2 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cnc[nH]2)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1079185 5810 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 438 8 2 4 4.2 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cnc[nH]2)CC3)cc1 10.1016/j.bmcl.2009.09.027
46882395 5811 0 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 452 8 2 4 4.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2[nH]cnc2C)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1079186 5811 0 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 452 8 2 4 4.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2[nH]cnc2C)CC3)cc1 10.1016/j.bmcl.2009.09.027
44570699 191281 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 474 5 2 5 2.2 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(NC(=O)c3ccccc3F)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL519121 191281 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 474 5 2 5 2.2 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(NC(=O)c3ccccc3F)cc2)C1 10.1016/j.bmcl.2008.12.042
69196498 88882 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)s1 10.6019/CHEMBL2364335
CHEMBL2364374 88882 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)s1 10.6019/CHEMBL2364335
69197028 88921 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)c3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364413 88921 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)c3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69198238 88932 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 5 2 5 4.7 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364423 88932 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 5 2 5 4.7 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
11712867 88969 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)cc1F 10.6019/CHEMBL2364335
CHEMBL2364459 88969 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)cc1F 10.6019/CHEMBL2364335
69194471 88984 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)c(F)c1 10.6019/CHEMBL2364335
CHEMBL2364473 88984 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)c(F)c1 10.6019/CHEMBL2364335
11698505 88993 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)c2)cc1 10.6019/CHEMBL2364335
CHEMBL2364482 88993 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)c2)cc1 10.6019/CHEMBL2364335
9950632 88677 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.05.100
CHEMBL236038 88677 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GHS receptorAgonist activity at GHS receptor
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.05.100
44579880 186811 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL489401 186811 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
44579841 192530 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccc(Cl)cc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL521176 192530 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccc(Cl)cc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44434010 88744 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 445 14 3 8 1.5 CCCCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
CHEMBL236311 88744 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 445 14 3 8 1.5 CCCCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2008.03.059
9950632 88677 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2007.07.099
9950632 88677 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.01.100
CHEMBL236038 88677 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2007.07.099
CHEMBL236038 88677 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.01.100
44434010 88744 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 445 14 3 8 1.5 CCCCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL236311 88744 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 445 14 3 8 1.5 CCCCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
44437966 202070 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 607 8 1 5 4.8 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N1CCOCC1)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
CHEMBL608827 202070 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 607 8 1 5 4.8 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N1CCOCC1)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
44437969 202496 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 565 8 1 4 5.0 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N(C)C)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
CHEMBL611488 202496 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 565 8 1 4 5.0 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N(C)C)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
44437966 202070 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 607 8 1 5 4.8 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N1CCOCC1)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
CHEMBL608827 202070 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 607 8 1 5 4.8 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N1CCOCC1)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
44437969 202496 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 565 8 1 4 5.0 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N(C)C)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
CHEMBL611488 202496 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 565 8 1 4 5.0 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N(C)C)cc2C(F)(F)F 10.1016/j.bmc.2007.01.057
44454368 95233 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCC(C#N)c2ccccc2)n1 10.1016/j.bmcl.2008.01.100
CHEMBL256236 95233 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 447 11 2 8 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCC(C#N)c2ccccc2)n1 10.1016/j.bmcl.2008.01.100
145987684 167253 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 615 6 1 4 7.8 CC[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4293331 167253 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 615 6 1 4 7.8 CC[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
44444560 154930 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 541 5 1 5 3.4 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)Cc1cccc(I)c1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL401133 154930 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 541 5 1 5 3.4 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)Cc1cccc(I)c1)CC2 10.1016/j.bmcl.2007.09.067
145953855 162491 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4167669 162491 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
44570923 183932 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 403 4 1 5 2.0 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccco3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL481602 183932 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 403 4 1 5 2.0 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccco3)cc2)C1 10.1016/j.bmcl.2008.12.042
44570761 189948 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 413 4 1 4 2.5 NC1CCN(C(=O)C2CCCCN2S(=O)(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL517081 189948 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 413 4 1 4 2.5 NC1CCN(C(=O)C2CCCCN2S(=O)(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
122178179 121237 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1002 29 10 9 3.8 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
CHEMBL3578008 121237 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1002 29 10 9 3.8 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
24969112 88847 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 445 5 2 7 3.2 Cc1ccc(-c2ccc(S(=O)(=O)Nc3ccnc(N4C[C@H](C)N[C@H](C)C4)n3)cc2F)o1 10.6019/CHEMBL2364335
CHEMBL2364339 88847 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 445 5 2 7 3.2 Cc1ccc(-c2ccc(S(=O)(=O)Nc3ccnc(N4C[C@H](C)N[C@H](C)C4)n3)cc2F)o1 10.6019/CHEMBL2364335
11540248 88853 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 479 5 2 6 4.9 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364345 88853 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 479 5 2 6 4.9 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11647560 88855 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 425 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2cccc3ccccc23)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364347 88855 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 425 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2cccc3ccccc23)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69196005 88886 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1sc2ccc(F)cc2c1C 10.6019/CHEMBL2364335
CHEMBL2364378 88886 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 5 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1sc2ccc(F)cc2c1C 10.6019/CHEMBL2364335
69198434 88894 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 488 7 2 8 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnccc2OC)s1 10.6019/CHEMBL2364335
CHEMBL2364386 88894 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 488 7 2 8 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnccc2OC)s1 10.6019/CHEMBL2364335
69198286 88902 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 401 4 2 5 3.9 C[C@H]1CN(c2cccc(NS(=O)(=O)c3cc4ccccc4s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364394 88902 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 401 4 2 5 3.9 C[C@H]1CN(c2cccc(NS(=O)(=O)c3cc4ccccc4s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11562181 88913 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 487 6 2 5 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(F)c3F)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364405 88913 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 487 6 2 5 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(F)c3F)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69196132 88924 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(F)c2)s1 10.6019/CHEMBL2364335
CHEMBL2364416 88924 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(F)c2)s1 10.6019/CHEMBL2364335
69197703 88925 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)cc2)s1 10.6019/CHEMBL2364335
CHEMBL2364417 88925 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)cc2)s1 10.6019/CHEMBL2364335
69194443 88946 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 487 6 2 5 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(F)c2F)cc1 10.6019/CHEMBL2364335
CHEMBL2364436 88946 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 487 6 2 5 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(F)c2F)cc1 10.6019/CHEMBL2364335
11503069 88949 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 439 5 2 4 4.5 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccccc4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364439 88949 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 439 5 2 4 4.5 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccccc4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
11647941 88956 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.4 Cc1cc(-c2ccoc2)ccc1S(=O)(=O)Nc1cc(N2C[C@H](C)N[C@H](C)C2)ccc1F 10.6019/CHEMBL2364335
CHEMBL2364446 88956 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.4 Cc1cc(-c2ccoc2)ccc1S(=O)(=O)Nc1cc(N2C[C@H](C)N[C@H](C)C2)ccc1F 10.6019/CHEMBL2364335
11576203 88963 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 6 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2c(c1)CCC(C)(C)O2 10.6019/CHEMBL2364335
CHEMBL2364453 88963 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 6 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2c(c1)CCC(C)(C)O2 10.6019/CHEMBL2364335
11683891 88977 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 453 6 2 7 3.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnccn2)cc1 10.6019/CHEMBL2364335
CHEMBL2364467 88977 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 453 6 2 7 3.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnccn2)cc1 10.6019/CHEMBL2364335
69194380 89001 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 6 2 6 4.0 COc1ccc(N2CCN[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364490 89001 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 6 2 6 4.0 COc1ccc(N2CCN[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
56926783 69029 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 470 4 3 4 2.8 CC[C@H](C)[C@@H]1NCCCC/C=C/CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923632 69029 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 470 4 3 4 2.8 CC[C@H](C)[C@@H]1NCCCC/C=C/CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
156021183 178100 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648308 178100 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156017268 177626 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641472 177626 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156021183 178100 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648308 178100 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)CC[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44453070 95064 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 453 6 2 7 3.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cncnc2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL255401 95064 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 453 6 2 7 3.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cncnc2)cc1 10.1016/j.bmcl.2007.12.021
44453097 155069 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 452 6 2 6 3.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccncc2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL401891 155069 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 452 6 2 6 3.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccncc2)cc1 10.1016/j.bmcl.2007.12.021
44570762 183404 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 414 4 1 5 1.9 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3cccnc3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL479865 183404 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 414 4 1 5 1.9 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3cccnc3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL3578013 211741 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
156017268 177626 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641472 177626 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44434114 89389 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 452 10 2 9 1.5 COC(=O)C(c1ccccc1)n1nnc([C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)n1 10.1016/j.bmcl.2007.07.099
CHEMBL237060 89389 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 452 10 2 9 1.5 COC(=O)C(c1ccccc1)n1nnc([C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)n1 10.1016/j.bmcl.2007.07.099
44450134 161868 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 479 13 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCc1ccccc1 10.1016/j.bmcl.2008.03.059
CHEMBL415095 161868 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 479 13 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCc1ccccc1 10.1016/j.bmcl.2008.03.059
44446177 94618 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252448 94618 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL500468 214092 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/s0960-894x(01)00324-9
44450105 95773 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 507 15 3 8 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCc1ccccc1 10.1016/j.bmcl.2008.03.059
CHEMBL258762 95773 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 507 15 3 8 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCc1ccccc1 10.1016/j.bmcl.2008.03.059
44447848 94871 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 547 15 4 11 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccc(OC(F)(F)F)cc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254167 94871 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 547 15 4 11 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccc(OC(F)(F)F)cc1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44580031 193046 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 381 7 2 4 3.2 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL522446 193046 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 381 7 2 4 3.2 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL3578013 211741 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
44447845 94849 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 599 14 4 10 2.3 CC(C)(N)C(=O)N[C@H](COCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL253966 94849 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 599 14 4 10 2.3 CC(C)(N)C(=O)N[C@H](COCc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44434119 89877 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 400 10 3 10 -0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1nnn[nH]1 10.1016/j.bmcl.2007.07.099
CHEMBL237925 89877 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 400 10 3 10 -0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1nnn[nH]1 10.1016/j.bmcl.2007.07.099
145953855 162491 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4167669 162491 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
44434121 89879 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 385 11 2 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCC#N 10.1016/j.bmcl.2007.07.099
CHEMBL237927 89879 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 385 11 2 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCC#N 10.1016/j.bmcl.2007.07.099
162646324 179712 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 688 17 3 9 4.8 CCN(CC)CCc1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(OC)cc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4744139 179712 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 688 17 3 9 4.8 CCN(CC)CCc1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(OC)cc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
10721075 15521 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 534 11 2 5 3.8 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1csc2ccccc12)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL121960 15521 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 534 11 2 5 3.8 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1csc2ccccc12)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
145959787 162261 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 162261 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
16114289 98637 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCNC2)cc1 10.1021/jm0704550
CHEMBL277376 98637 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCNC2)cc1 10.1021/jm0704550
56926892 69033 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923636 69033 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
145984632 166367 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 629 5 1 4 8.0 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)C(C)(C)C2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4276775 166367 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 629 5 1 4 8.0 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)C(C)(C)C2)ncn1 10.1021/acs.jmedchem.8b00794
155551597 173925 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 974 27 13 11 -1.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4541252 173925 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 974 27 13 11 -1.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
22862448 97149 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CC(=O)c1ccccc1O2 10.1016/s0960-894x(97)10199-8
CHEMBL268231 97149 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CC(=O)c1ccccc1O2 10.1016/s0960-894x(97)10199-8
22867465 97190 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)Cc1ccccc1C2 10.1016/s0960-894x(97)10199-8
CHEMBL268518 97190 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)Cc1ccccc1C2 10.1016/s0960-894x(97)10199-8
44301387 11232 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1179088 11232 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL59572 11232 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
56926356 68990 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923512 68990 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
10143731 64298 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 543 11 2 5 4.7 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)C(O)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181156 64298 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 543 11 2 5 4.7 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)C(O)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
44444558 167753 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 465 4 0 5 4.1 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(S(=O)(=O)c1ccc3ccccc3c1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL430398 167753 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 465 4 0 5 4.1 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(S(=O)(=O)c1ccc3ccccc3c1)CC2 10.1016/j.bmcl.2007.09.067
145959007 162233 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163623 162233 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
145959787 162261 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 162261 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
156021766 178103 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648355 178103 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44452826 95353 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 428 5 2 6 3.8 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
CHEMBL256809 95353 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 428 5 2 6 3.8 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
44452777 96191 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 470 6 2 7 4.0 CC(=O)c1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
CHEMBL260831 96191 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 470 6 2 7 4.0 CC(=O)c1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
11554351 96510 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 458 6 2 6 2.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(N2CCCC2=O)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL262879 96510 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 458 6 2 6 2.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(N2CCCC2=O)cc1 10.1016/j.bmcl.2007.12.021
11605061 96685 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 462 5 2 6 4.5 C[C@H]1CN(c2ccc(Cl)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
CHEMBL264170 96685 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 462 5 2 6 4.5 C[C@H]1CN(c2ccc(Cl)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
44452825 155226 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 472 7 2 7 4.2 CCOc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
CHEMBL402772 155226 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 472 7 2 7 4.2 CCOc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1 10.1016/j.bmcl.2007.12.021
CHEMBL3578017 211745 0 None -3 2 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
69197033 88878 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 442 6 2 7 3.3 COc1ccc(NS(=O)(=O)c2ccc(-c3cnco3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364370 88878 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 442 6 2 7 3.3 COc1ccc(NS(=O)(=O)c2ccc(-c3cnco3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69197513 88893 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 448 6 2 8 3.4 COc1ccc(NS(=O)(=O)c2ccc(-c3cnco3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364385 88893 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 448 6 2 8 3.4 COc1ccc(NS(=O)(=O)c2ccc(-c3cnco3)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69196509 88897 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 467 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2C)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364389 88897 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 467 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2C)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11669948 88909 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 467 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2ccc(Br)c(C)c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364401 88909 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 467 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2ccc(Br)c(C)c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69196071 88967 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 478 6 2 8 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)n2)s1 10.6019/CHEMBL2364335
CHEMBL2364457 88967 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 478 6 2 8 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)n2)s1 10.6019/CHEMBL2364335
69194899 88971 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2ccoc2)c1 10.6019/CHEMBL2364335
CHEMBL2364461 88971 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2ccoc2)c1 10.6019/CHEMBL2364335
44434055 89276 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL236858 89276 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
44436889 153033 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 563 11 3 5 6.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCCCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL397594 153033 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 563 11 3 5 6.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCCCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44570922 192539 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 415 3 1 4 1.6 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL521264 192539 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 415 3 1 4 1.6 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(Br)cc2)C1 10.1016/j.bmcl.2008.12.042
69196838 88858 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 426 5 2 6 3.2 COc1ccc(NS(=O)(=O)c2cccc3cccnc23)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364350 88858 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 426 5 2 6 3.2 COc1ccc(NS(=O)(=O)c2cccc3cccnc23)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
25211977 186878 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 C[C@H](Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL489818 186878 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 C[C@H](Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
16113580 137854 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm701292s
CHEMBL376258 137854 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at GHSR1a expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm701292s
44434111 146258 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1cc2ccccc2n1S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL392077 146258 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1cc2ccccc2n1S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
15481185 77232 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
CHEMBL207970 77232 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1016/j.bmc.2007.01.057
127048059 139541 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 675 16 6 8 4.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797225 139541 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 675 16 6 8 4.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
16113580 137854 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL376258 137854 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
44450103 95743 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 495 14 3 10 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCS(C)(=O)=O 10.1016/j.bmcl.2008.03.059
CHEMBL258551 95743 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 495 14 3 10 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCS(C)(=O)=O 10.1016/j.bmcl.2008.03.059
44391032 64815 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 513 8 1 5 5.7 CC(C)N(CCNC(=O)C1c2ccc(Oc3cccc(F)c3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL182050 64815 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 513 8 1 5 5.7 CC(C)N(CCNC(=O)C1c2ccc(Oc3cccc(F)c3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
156011736 177399 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 605 7 3 7 3.0 Cc1oc(-c2ccc(C(F)(F)F)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4638566 177399 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 605 7 3 7 3.0 Cc1oc(-c2ccc(C(F)(F)F)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
44450132 95983 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 447 14 4 9 0.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCNC(=O)CCCCO 10.1016/j.bmcl.2008.03.059
CHEMBL259712 95983 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 447 14 4 9 0.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCNC(=O)CCCCO 10.1016/j.bmcl.2008.03.059
145948725 167473 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 885 20 7 9 6.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL4299615 167473 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 885 20 7 9 6.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
44281450 99617 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 573 12 3 8 1.5 COC(=O)CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
CHEMBL284295 99617 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 573 12 3 8 1.5 COC(=O)CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
44281450 99617 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 573 12 3 8 1.5 COC(=O)CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
CHEMBL284295 99617 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 573 12 3 8 1.5 COC(=O)CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1 10.1016/j.bmc.2007.01.057
44411584 10271 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161822 10271 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
156015766 177544 0 None 407 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 7 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4640438 177544 0 None 407 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 7 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2)on1 10.1021/acs.jmedchem.0c00828
44411584 10271 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161822 10271 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
22888433 64583 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 535 10 1 5 5.9 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC1CCCCC1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181735 64583 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 535 10 1 5 5.9 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC1CCCCC1)C(C)C 10.1016/j.bmcl.2005.02.040
44579775 187156 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 352 7 1 3 3.5 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1ccccc1 10.1016/j.bmcl.2008.07.120
CHEMBL492230 187156 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 352 7 1 3 3.5 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1ccccc1 10.1016/j.bmcl.2008.07.120
11258291 189080 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1Cl)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL510195 189080 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1Cl)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44579882 193042 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL522426 193042 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
44450044 161078 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 433 13 4 9 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCO 10.1016/j.bmcl.2008.03.059
CHEMBL411699 161078 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 433 13 4 9 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCO 10.1016/j.bmcl.2008.03.059
56926463 69009 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923611 69009 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
145981687 166553 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 509 5 1 3 6.5 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(Cl)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4279987 166553 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 509 5 1 3 6.5 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(Cl)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
44579640 186872 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 354 7 1 4 3.2 COc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
CHEMBL489793 186872 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 354 7 1 4 3.2 COc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
44579686 186967 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 395 8 2 4 3.6 CCC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(NC(C)=O)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL490614 186967 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 395 8 2 4 3.6 CCC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(NC(C)=O)cc1 10.1016/j.bmcl.2008.07.120
16203238 137084 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 531 9 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1 10.1021/jm070024h
CHEMBL374757 137084 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 531 9 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1 10.1021/jm070024h
44390997 122975 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 481 8 1 5 4.6 CC(C)N(C)CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL360891 122975 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 481 8 1 5 4.6 CC(C)N(C)CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL3578017 211745 0 None -3 2 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
23661656 169020 0 None -7 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 564 8 1 4 5.3 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
CHEMBL439560 169020 0 None -7 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 564 8 1 4 5.3 CC(C)C[C@H](N)c1cc(C(F)(F)F)ccc1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2)N2CCCC2=O)CC1 10.1016/j.bmc.2007.05.026
44434074 154649 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL399625 154649 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
44434009 167429 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 431 13 3 8 1.1 CCCCNC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL429799 167429 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 431 13 3 8 1.1 CCCCNC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
22867312 23838 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 472 5 3 4 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)Cc1ccccc1C2=O 10.1016/s0960-894x(97)10199-8
CHEMBL13366 23838 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 472 5 3 4 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)Cc1ccccc1C2=O 10.1016/s0960-894x(97)10199-8
162665952 182355 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 688 14 4 10 3.5 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4785149 182355 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 688 14 4 10 3.5 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
44434056 144970 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL391088 144970 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
44434007 88546 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 390 10 2 9 0.3 COC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL235446 88546 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 390 10 2 9 0.3 COC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
156021766 178103 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648355 178103 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44391035 122582 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 545 11 1 4 5.3 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)Cc1ccccc1F)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL360247 122582 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 545 11 1 4 5.3 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)Cc1ccccc1F)C(C)C 10.1016/j.bmcl.2005.02.040
44301512 11990 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 566 13 3 8 1.0 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@@H](N)CO)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1183340 11990 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 566 13 3 8 1.0 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@@H](N)CO)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL291333 11990 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 566 13 3 8 1.0 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@@H](N)CO)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
145979268 166640 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 607 8 1 5 7.4 COc1ccc([C@H](CC2CC2)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4281647 166640 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 607 8 1 5 7.4 COc1ccc([C@H](CC2CC2)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
145959007 162233 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163623 162233 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
44580030 186946 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 324 6 1 3 3.2 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccccc1 10.1016/j.bmcl.2008.07.120
CHEMBL490422 186946 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 324 6 1 3 3.2 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccccc1 10.1016/j.bmcl.2008.07.120
118718706 115353 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL3350011 115353 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
44301462 11230 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1179075 11230 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL58758 11230 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
16113800 137787 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 536 11 3 6 4.7 COc1cccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL375972 137787 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 536 11 3 6 4.7 COc1cccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
44391015 123529 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 1 5 5.2 COc1ccc(CC(=O)N2CCc3cc(OCc4ccccc4)ccc3C2C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
CHEMBL361802 123529 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 1 5 5.2 COc1ccc(CC(=O)N2CCc3cc(OCc4ccccc4)ccc3C2C(=O)NCCN(C(C)C)C(C)C)cc1 10.1016/j.bmcl.2005.02.040
162677268 183549 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 663 14 3 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4800459 183549 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 663 14 3 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
10507433 16435 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 578 13 3 6 3.5 C[C@H](O)CNC(=O)[C@@H](Cc1cccs1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL123430 16435 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 578 13 3 6 3.5 C[C@H](O)CNC(=O)[C@@H](Cc1cccs1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
23730458 146547 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 499 14 3 11 0.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCn1ccnc1 10.1021/jm7010595
CHEMBL392296 146547 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 499 14 3 11 0.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCn1ccnc1 10.1021/jm7010595
44576247 214199 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL506986 214199 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
168285897 191633 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 273 7 1 2 4.1 CCCCCCCc1cc(=O)c2cc(OC)ccc2[nH]1 10.1021/acs.jmedchem.1c02191
CHEMBL5196194 191633 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 273 7 1 2 4.1 CCCCCCCc1cc(=O)c2cc(OC)ccc2[nH]1 10.1021/acs.jmedchem.1c02191
155529391 171416 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1427 41 20 17 -3.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4463042 171416 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1427 41 20 17 -3.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
145956659 162031 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4160434 162031 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
155537651 172292 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1597 47 22 19 -3.8 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(N)=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4475293 172292 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1597 47 22 19 -3.8 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(N)=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
145981196 166512 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 627 5 1 6 7.1 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)N[C@@H](C)c4ccc(-c5cnccn5)c(Cl)c4Cl)CC3)C2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4279344 166512 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 627 5 1 6 7.1 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)N[C@@H](C)c4ccc(-c5cnccn5)c(Cl)c4Cl)CC3)C2)ncn1 10.1021/acs.jmedchem.8b00794
145979819 166449 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 655 8 1 6 7.9 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4278185 166449 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 655 8 1 6 7.9 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
44434016 90164 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 415 12 3 7 1.5 CCCCNC(=O)CCn1nnnc1[C@@H](CCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL238228 90164 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 415 12 3 7 1.5 CCCCNC(=O)CCn1nnnc1[C@@H](CCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
16113692 137211 1 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 559 11 4 5 5.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
CHEMBL375162 137211 1 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 559 11 4 5 5.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
24970113 69027 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 580 3 3 5 3.8 C[C@@H]1CN[C@@H](C2CCCCC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923629 69027 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 580 3 3 5 3.8 C[C@@H]1CN[C@@H](C2CCCCC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL2170777 209342 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CCC[C@H](NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm300414b
145956026 162638 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4169979 162638 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
22862436 10282 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161834 10282 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
10602640 138164 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1016/j.bmc.2007.01.057
CHEMBL376970 138164 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1016/j.bmc.2007.01.057
10791616 139511 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL379564 139511 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
10029990 169260 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL441360 169260 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
11526696 71573 17 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release incubated for 3 mins by FLIPR assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release incubated for 3 mins by FLIPR assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
CHEMBL1923502 71573 17 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release incubated for 3 mins by FLIPR assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release incubated for 3 mins by FLIPR assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
CHEMBL1963249 71573 17 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release incubated for 3 mins by FLIPR assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release incubated for 3 mins by FLIPR assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 nan
10649323 15498 0 None - 1 Rat 8.3 pEC50 = 8.3 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 508 13 2 5 2.5 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](COCc1ccccc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL121803 15498 0 None - 1 Rat 8.3 pEC50 = 8.3 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 508 13 2 5 2.5 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](COCc1ccccc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
10841400 16819 0 None - 1 Rat 8.3 pEC50 = 8.3 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 608 13 3 5 3.7 C[C@H](O)CNC(=O)[C@@H](Cc1ccc(F)c(F)c1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL124831 16819 0 None - 1 Rat 8.3 pEC50 = 8.3 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 608 13 3 5 3.7 C[C@H](O)CNC(=O)[C@@H](Cc1ccc(F)c(F)c1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
156009875 177099 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633695 177099 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44444562 94442 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 463 6 1 5 3.5 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)CCc1ccccc1Cl)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL251365 94442 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 463 6 1 5 3.5 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)CCc1ccccc1Cl)CC2 10.1016/j.bmcl.2007.09.067
145956026 162638 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4169979 162638 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
22862436 10282 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161834 10282 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
10602640 138164 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1016/j.bmc.2007.01.057
CHEMBL376970 138164 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1016/j.bmc.2007.01.057
10791616 139511 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL379564 139511 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
10029990 169260 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL441360 169260 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
156009875 177099 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633695 177099 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156015766 177544 0 None 407 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 7 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2)on1 10.1021/acs.jmedchem.0c00828
CHEMBL4640438 177544 0 None 407 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 523 7 3 7 1.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(-c2ccccc2)on1 10.1021/acs.jmedchem.0c00828
44570967 190145 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 437 4 2 6 1.1 Cc1ccc(-c2ccc(S(=O)(=O)N3C[C@@H](O)C[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
CHEMBL517391 190145 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 437 4 2 6 1.1 Cc1ccc(-c2ccc(S(=O)(=O)N3C[C@@H](O)C[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1 10.1016/j.bmcl.2008.12.042
24969114 88850 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 506 6 2 7 4.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)nc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)cc1Cl 10.6019/CHEMBL2364335
CHEMBL2364342 88850 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 506 6 2 7 4.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)nc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)cc1Cl 10.6019/CHEMBL2364335
59007076 88873 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)cc1 10.6019/CHEMBL2364335
CHEMBL2364365 88873 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 457 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)cc1 10.6019/CHEMBL2364335
69197196 88875 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)s1 10.6019/CHEMBL2364335
CHEMBL2364367 88875 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 463 6 2 7 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)s1 10.6019/CHEMBL2364335
69197071 88914 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 445 5 2 5 4.5 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364406 88914 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 445 5 2 5 4.5 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69194482 88929 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 409 4 2 4 4.1 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2ccccc2c1 10.6019/CHEMBL2364335
CHEMBL2364420 88929 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 409 4 2 4 4.1 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2ccccc2c1 10.6019/CHEMBL2364335
11719784 88966 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)cc1C 10.6019/CHEMBL2364335
CHEMBL2364456 88966 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)cc1C 10.6019/CHEMBL2364335
59007054 88998 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 5 3 6 3.9 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3O)cc2)o1 10.6019/CHEMBL2364335
CHEMBL2364487 88998 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 5 3 6 3.9 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3O)cc2)o1 10.6019/CHEMBL2364335
16114097 79128 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCCNC2)c(OC)c1 10.1021/jm0704550
CHEMBL2113321 79128 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCCNC2)c(OC)c1 10.1021/jm0704550
16113710 79132 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCNCC1 10.1021/jm0704550
CHEMBL2113325 79132 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCNCC1 10.1021/jm0704550
23730226 147847 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 449 13 4 10 -0.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCO 10.1021/jm7010595
CHEMBL393329 147847 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 449 13 4 10 -0.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCO 10.1021/jm7010595
71453489 209345 15 None - 1 Human 8.3 pEC50 = 8.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.8b01644
CHEMBL2170781 209345 15 None - 1 Human 8.3 pEC50 = 8.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.8b01644
44411632 10272 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161823 10272 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
22888425 62494 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 2 5 4.7 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)C(CO)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL178216 62494 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 2 5 4.7 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)C(CO)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
44411632 10272 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161823 10272 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL2170782 209346 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1csc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44579858 186901 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2Cl)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL490010 186901 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2Cl)cc1 10.1016/j.bmcl.2008.07.120
44579778 186995 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1)C(=O)N(Cc1cccc(Cl)c1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL490801 186995 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1ccccc1)C(=O)N(Cc1cccc(Cl)c1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
162657606 181093 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 693 15 3 8 5.7 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4760409 181093 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 693 15 3 8 5.7 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
145956659 162031 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4160434 162031 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
145950987 162816 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 4 3 5 1.7 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCO3)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4172848 162816 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 4 3 5 1.7 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCO3)ccc21 10.1021/acs.jmedchem.8b00322
69198313 88869 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 426 5 2 6 3.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc2cccnc12 10.6019/CHEMBL2364335
CHEMBL2364361 88869 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 426 5 2 6 3.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc2cccnc12 10.6019/CHEMBL2364335
69195692 88870 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.6019/CHEMBL2364335
CHEMBL2364362 88870 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.6019/CHEMBL2364335
69196612 88871 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 442 6 2 7 3.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnco2)cc1 10.6019/CHEMBL2364335
CHEMBL2364363 88871 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 442 6 2 7 3.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnco2)cc1 10.6019/CHEMBL2364335
11511158 88919 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccc3C)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364411 88919 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccc3C)s2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69198054 88972 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2cc(C)cs2)c1 10.6019/CHEMBL2364335
CHEMBL2364462 88972 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2cc(C)cs2)c1 10.6019/CHEMBL2364335
69195074 88985 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)nc1 10.6019/CHEMBL2364335
CHEMBL2364474 88985 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)nc1 10.6019/CHEMBL2364335
69195546 88995 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Cl)c2ccccc12 10.6019/CHEMBL2364335
CHEMBL2364484 88995 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 459 5 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Cl)c2ccccc12 10.6019/CHEMBL2364335
44580028 193226 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 416 8 1 4 4.5 COc1c(-c2ccccc2)cccc1N(C[C@H]1CCCN1)C(=O)COc1ccccc1 10.1016/j.bmcl.2008.07.120
CHEMBL523786 193226 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 416 8 1 4 4.5 COc1c(-c2ccccc2)cccc1N(C[C@H]1CCCN1)C(=O)COc1ccccc1 10.1016/j.bmcl.2008.07.120
44434011 147839 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 465 12 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL393321 147839 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 465 12 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCc1ccccc1 10.1016/j.bmcl.2007.07.099
57390496 69026 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
CHEMBL1923628 69026 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
145988894 167120 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4290680 167120 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
44434086 148831 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 420 10 2 7 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C/C=C/c2ccccc2)n1 10.1016/j.bmcl.2007.07.099
CHEMBL394130 148831 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 420 10 2 7 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C/C=C/c2ccccc2)n1 10.1016/j.bmcl.2007.07.099
145950987 162816 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 4 3 5 1.7 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCO3)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4172848 162816 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 418 4 3 5 1.7 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCO3)ccc21 10.1021/acs.jmedchem.8b00322
44449924 159921 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 487 12 4 9 1.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)N[C@H]1CC[C@H](O)CC1 10.1016/j.bmcl.2008.03.059
CHEMBL410730 159921 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 487 12 4 9 1.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)N[C@H]1CC[C@H](O)CC1 10.1016/j.bmcl.2008.03.059
56926785 69031 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923634 69031 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
44434078 89881 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 513 10 2 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CC2Cc3ccccc3N2S(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL237932 89881 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 513 10 2 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CC2Cc3ccccc3N2S(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
44434008 146509 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 404 11 2 9 0.7 COC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL392268 146509 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 404 11 2 9 0.7 COC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
44411913 10281 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161833 10281 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
44268939 30416 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@]2(CC(=O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
CHEMBL13926 30416 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@]2(CC(=O)c3ccccc3O2)C1 10.1016/s0960-894x(97)10199-8
44411913 10281 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161833 10281 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1016/j.bmc.2007.01.057
44434015 88462 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 493 14 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL235011 88462 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 493 14 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCCc1ccccc1 10.1016/j.bmcl.2007.07.099
44411905 10280 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161832 10280 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
10506325 101214 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1016/j.bmc.2007.01.057
CHEMBL296104 101214 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1016/j.bmc.2007.01.057
16113371 79124 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL2113318 79124 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
162676229 183280 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 715 15 3 10 3.9 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4797064 183280 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 715 15 3 10 3.9 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL3578005 211736 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1021/jm501702q
44348031 113062 0 None - 1 Rat 8.2 pEC50 = 8.2 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 618 14 3 5 4.3 C[C@@H](O)CNC(=O)[C@@H](Cc1ccc(F)cc1)N(C)C(=O)[C@@H](CC1=CCC(c2ccccc2)C=C1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL331303 113062 0 None - 1 Rat 8.2 pEC50 = 8.2 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 618 14 3 5 4.3 C[C@@H](O)CNC(=O)[C@@H](Cc1ccc(F)cc1)N(C)C(=O)[C@@H](CC1=CCC(c2ccccc2)C=C1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
44411905 10280 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161832 10280 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1016/j.bmc.2007.01.057
44437953 10292 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 522 9 3 6 1.5 NCCNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCN1C(=O)CCS(=O)(=O)c2ccccc21 10.1016/j.bmc.2007.01.057
CHEMBL1162062 10292 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 522 9 3 6 1.5 NCCNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCN1C(=O)CCS(=O)(=O)c2ccccc21 10.1016/j.bmc.2007.01.057
10506325 101214 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1016/j.bmc.2007.01.057
CHEMBL296104 101214 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1016/j.bmc.2007.01.057
44436857 145631 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 594 12 4 7 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL391588 145631 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 594 12 4 7 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
156021787 178119 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648799 178119 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
10006735 116987 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 515 10 3 6 2.0 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(C)(=O)=O)CC1 10.1016/j.bmc.2007.01.057
CHEMBL33892 116987 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 515 10 3 6 2.0 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(C)(=O)=O)CC1 10.1016/j.bmc.2007.01.057
10006735 116987 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 515 10 3 6 2.0 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(C)(=O)=O)CC1 10.1016/j.bmc.2007.01.057
CHEMBL33892 116987 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 515 10 3 6 2.0 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(C)(=O)=O)CC1 10.1016/j.bmc.2007.01.057
156021787 178119 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648799 178119 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 509 6 4 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)N[C@@H]3CCCNC3)cc2c1 10.1021/acs.jmedchem.0c00828
11712108 161284 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 451 6 2 5 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL412303 161284 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 451 6 2 5 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2007.12.021
44571003 192564 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 445 4 1 5 3.0 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3C[C@H](C)N[C@H](C)C3)cc2)o1 10.1016/j.bmcl.2008.12.042
CHEMBL521439 192564 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 445 4 1 5 3.0 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3C[C@H](C)N[C@H](C)C3)cc2)o1 10.1016/j.bmcl.2008.12.042
CHEMBL3578005 211736 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1021/jm501702q
69196876 88860 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 7 2.9 COc1ccc(NS(=O)(=O)c2ccc(-n3cccn3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364352 88860 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 7 2.9 COc1ccc(NS(=O)(=O)c2ccc(-n3cccn3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11562329 88899 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 495 8 2 6 4.5 COCc1cccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)cc2)c1 10.6019/CHEMBL2364335
CHEMBL2364391 88899 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 495 8 2 6 4.5 COCc1cccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)cc2)c1 10.6019/CHEMBL2364335
69196868 88903 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 427 5 2 5 4.4 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-c4cccs4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364395 88903 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 427 5 2 5 4.4 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-c4cccs4)cc3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69196990 88959 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 480 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)cc1C 10.6019/CHEMBL2364335
CHEMBL2364449 88959 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 480 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)cc1C 10.6019/CHEMBL2364335
69195880 88976 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 6 5.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)c(C)c1 10.6019/CHEMBL2364335
CHEMBL2364466 88976 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 485 6 2 6 5.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)c(C)c1 10.6019/CHEMBL2364335
11518463 88979 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1cc(-c2cc(C)cs2)ccc1S(=O)(=O)Nc1cccc(N2C[C@H](C)N[C@H](C)C2)c1 10.6019/CHEMBL2364335
CHEMBL2364469 88979 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1cc(-c2cc(C)cs2)ccc1S(=O)(=O)Nc1cccc(N2C[C@H](C)N[C@H](C)C2)c1 10.6019/CHEMBL2364335
69195024 89003 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 461 5 3 6 4.2 C[C@H]1CN(c2ccc(O)c(NS(=O)(=O)c3ccc(-c4ccccc4F)s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364492 89003 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 461 5 3 6 4.2 C[C@H]1CN(c2ccc(O)c(NS(=O)(=O)c3ccc(-c4ccccc4F)s3)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
44390922 122120 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 1 5 5.2 COc1cccc(CC(=O)N2CCc3cc(OCc4ccccc4)ccc3C2C(=O)NCCN(C(C)C)C(C)C)c1 10.1016/j.bmcl.2005.02.040
CHEMBL359686 122120 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 557 12 1 5 5.2 COc1cccc(CC(=O)N2CCc3cc(OCc4ccccc4)ccc3C2C(=O)NCCN(C(C)C)C(C)C)c1 10.1016/j.bmcl.2005.02.040
23631026 167432 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant GHSR1a expressed in HEK293F cells assessed as stimulation of [35S]GTP-gamma-S binding relative to ghrelinAgonist activity at human recombinant GHSR1a expressed in HEK293F cells assessed as stimulation of [35S]GTP-gamma-S binding relative to ghrelin
ChEMBL 443 5 1 5 5.3 Cc1ccccc1-c1nc2ccc(Oc3ccc(F)cc3)cc2c(=O)n1CC1CCCNC1 10.1021/jm070071+
CHEMBL429817 167432 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human recombinant GHSR1a expressed in HEK293F cells assessed as stimulation of [35S]GTP-gamma-S binding relative to ghrelinAgonist activity at human recombinant GHSR1a expressed in HEK293F cells assessed as stimulation of [35S]GTP-gamma-S binding relative to ghrelin
ChEMBL 443 5 1 5 5.3 Cc1ccccc1-c1nc2ccc(Oc3ccc(F)cc3)cc2c(=O)n1CC1CCCNC1 10.1021/jm070071+
CHEMBL2170779 209343 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at FLAG-tagged human ghrelin receptor Ser123:Ala mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at FLAG-tagged human ghrelin receptor Ser123:Ala mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44447842 94990 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.6 CC(C)(N)C(=O)N[C@H](COCc1cc(Cl)cc(Cl)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
CHEMBL254972 94990 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Inhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assayInhibition of human growth hormone secretagogue receptor assessed as measuring intracellular calcium level by FLIPR assay
ChEMBL 531 14 4 10 1.6 CC(C)(N)C(=O)N[C@H](COCc1cc(Cl)cc(Cl)c1)c1nnnn1CCOC(=O)NCCCCO 10.1016/j.bmcl.2008.02.021
44579804 187041 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(Cc1ccc(Cl)cc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL491220 187041 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 406 7 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(Cc1ccc(Cl)cc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
145948708 167472 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 886 20 7 10 5.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CNCCO3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL4299606 167472 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 886 20 7 10 5.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CNCCO3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
121879 2222 24 None 1 5 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1016/s0960-894x(97)10199-8
5868 2222 24 None 1 5 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1016/s0960-894x(97)10199-8
CHEMBL308716 2222 24 None 1 5 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1016/s0960-894x(97)10199-8
44268996 166439 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(Cc3ccccc3C2)C1 10.1016/s0960-894x(97)10199-8
CHEMBL427806 166439 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(Cc3ccccc3C2)C1 10.1016/s0960-894x(97)10199-8
122178180 121238 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1130 35 12 11 3.4 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
CHEMBL3578009 121238 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1130 35 12 11 3.4 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
44579959 184248 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL483865 184248 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(Cl)cc1 10.1016/j.bmcl.2008.07.120
44454117 155532 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
CHEMBL404336 155532 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
162677361 183485 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 685 16 4 8 4.7 COc1ccc(C[C@@H](N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4799766 183485 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 685 16 4 8 4.7 COc1ccc(C[C@@H](N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL2170700 209337 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc(C(C)(C)C)cc1)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44444570 154744 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 456 5 1 7 3.0 COc1cc2c(cc1N1CCNCC1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL400125 154744 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
ChEMBL 456 5 1 7 3.0 COc1cc2c(cc1N1CCNCC1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2 10.1016/j.bmcl.2007.09.067
156017532 177884 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645072 177884 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
11662746 97785 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 467 7 2 6 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.12.021
CHEMBL271947 97785 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 467 7 2 6 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Oc2ccccc2)cc1 10.1016/j.bmcl.2007.12.021
122178180 121238 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1130 35 12 11 3.4 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
CHEMBL3578009 121238 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL 1130 35 12 11 3.4 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O 10.1021/jm501702q
CHEMBL3578007 211738 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm501702q
16750162 88849 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 474 6 2 7 3.8 COc1ncc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)c(F)c1 10.6019/CHEMBL2364335
CHEMBL2364341 88849 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 474 6 2 7 3.8 COc1ncc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)c(F)c1 10.6019/CHEMBL2364335
11568467 88859 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.0 COc1ccc(NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364351 88859 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 443 5 2 5 4.0 COc1ccc(NS(=O)(=O)c2ccc(Cl)c(Cl)c2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69197136 88960 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc(C)c(-c2ccccc2F)s1 10.6019/CHEMBL2364335
CHEMBL2364450 88960 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc(C)c(-c2ccccc2F)s1 10.6019/CHEMBL2364335
69195304 88974 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 455 4 2 4 3.9 Cc1cc(S(=O)(=O)Nc2cc(N3C[C@H](C)N[C@H](C)C3)ccc2F)ccc1Br 10.6019/CHEMBL2364335
CHEMBL2364464 88974 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 455 4 2 4 3.9 Cc1cc(S(=O)(=O)Nc2cc(N3C[C@H](C)N[C@H](C)C3)ccc2F)ccc1Br 10.6019/CHEMBL2364335
145949880 162767 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4172217 162767 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
16114099 137199 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 559 10 4 5 5.5 Cc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL375103 137199 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 559 10 4 5 5.5 Cc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
44269018 97319 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CCc3ccccc32)C1 10.1016/s0960-894x(97)10199-8
CHEMBL269447 97319 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CCc3ccccc32)C1 10.1016/s0960-894x(97)10199-8
145949880 162767 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4172217 162767 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
156015598 177553 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 486 7 4 6 0.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(C2CC2)n[nH]1 10.1021/acs.jmedchem.0c00828
CHEMBL4640573 177553 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 486 7 4 6 0.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(C2CC2)n[nH]1 10.1021/acs.jmedchem.0c00828
44452827 95397 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 453 5 2 7 3.7 C[C@H]1CN(c2cc(NS(=O)(=O)c3ccc(-c4ccccn4)s3)ccc2C#N)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
CHEMBL257019 95397 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 453 5 2 7 3.7 C[C@H]1CN(c2cc(NS(=O)(=O)c3ccc(-c4ccccn4)s3)ccc2C#N)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
46882582 5723 0 None -125 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 466 5 2 5 3.9 CC1(C)CCc2cc(S(=O)(=O)Nc3ccc4c(c3)CCN(Cc3cc[nH]n3)CC4)ccc2O1 10.1016/j.bmcl.2009.09.027
CHEMBL1078490 5723 0 None -125 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 466 5 2 5 3.9 CC1(C)CCc2cc(S(=O)(=O)Nc3ccc4c(c3)CCN(Cc3cc[nH]n3)CC4)ccc2O1 10.1016/j.bmcl.2009.09.027
145988647 167048 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4ncccn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4289530 167048 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4ncccn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
44454367 95232 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
CHEMBL256235 95232 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
16113691 136694 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm0704550
CHEMBL374073 136694 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm0704550
16113691 136694 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
CHEMBL374073 136694 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
22867380 29389 1 None - 1 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 472 5 3 3 3.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCCc3ccccc32)CC1 10.1016/s0960-894x(97)10199-8
CHEMBL13841 29389 1 None - 1 Rat 7.2 pEC50 = 7.2 Functional
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
ChEMBL 472 5 3 3 3.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCCc3ccccc32)CC1 10.1016/s0960-894x(97)10199-8
2098 3668 36 None -128 11 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02122
36511 3668 36 None -128 11 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02122
3805 3668 36 None -128 11 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02122
3835 3668 36 None -128 11 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02122
CHEMBL235363 3668 36 None -128 11 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02122
155561671 175640 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 817 22 11 9 -0.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4581511 175640 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 817 22 11 9 -0.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
44434073 89571 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL237507 89571 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
145981794 166672 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 567 6 1 5 6.6 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4282394 166672 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 567 6 1 5 6.6 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
56926173 68983 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm1012374
CHEMBL1923501 68983 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm1012374
44301389 11243 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1179118 11243 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL61292 11243 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
156015598 177553 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 486 7 4 6 0.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(C2CC2)n[nH]1 10.1021/acs.jmedchem.0c00828
CHEMBL4640573 177553 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 486 7 4 6 0.6 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1)c1cc(C2CC2)n[nH]1 10.1021/acs.jmedchem.0c00828
156017532 177884 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645072 177884 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
10100708 12002 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 530 9 3 7 0.3 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@@H](N)CO)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL1183387 12002 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 530 9 3 7 0.3 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@@H](N)CO)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL294408 12002 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 530 9 3 7 0.3 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@@H](N)CO)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
44579756 186799 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL489370 186799 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
145958487 162160 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc(F)c21 10.1021/acs.jmedchem.8b00322
CHEMBL4162545 162160 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc(F)c21 10.1021/acs.jmedchem.8b00322
156016840 177607 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 621 7 3 7 3.4 Cc1nc(-c2cccc(C(F)(F)F)c2)sc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4641215 177607 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 621 7 3 7 3.4 Cc1nc(-c2cccc(C(F)(F)F)c2)sc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL2170779 209343 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at FLAG-tagged human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at FLAG-tagged human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
71453489 209345 15 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Thr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Thr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 209345 15 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Thr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Thr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
10209618 63469 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 555 11 1 5 5.4 CC(=O)c1ccccc1C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL179978 63469 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 555 11 1 5 5.4 CC(=O)c1ccccc1C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
44391041 64291 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 591 11 1 6 5.1 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)S(=O)(=O)Cc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL181123 64291 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 591 11 1 6 5.1 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)S(=O)(=O)Cc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
10600702 141311 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL383526 141311 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
10600702 141311 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
CHEMBL383526 141311 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1016/j.bmc.2007.01.057
9868878 96512 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 460 14 4 9 -0.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCC(N)=O 10.1016/j.bmcl.2008.03.059
CHEMBL262884 96512 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 460 14 4 9 -0.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCC(N)=O 10.1016/j.bmcl.2008.03.059
11306502 63612 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180094 63612 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C 10.1016/j.bmcl.2005.02.040
22888395 63875 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 513 10 1 4 5.2 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180540 63875 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 513 10 1 4 5.2 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)c1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
156021942 178199 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4649860 178199 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
16113248 79135 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 560 11 3 5 5.6 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
CHEMBL2113328 79135 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 560 11 3 5 5.6 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
23730342 89873 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 511 13 4 10 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCc1cccc(O)c1 10.1021/jm7010595
CHEMBL237916 89873 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 511 13 4 10 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCc1cccc(O)c1 10.1021/jm7010595
145958487 162160 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc(F)c21 10.1021/acs.jmedchem.8b00322
CHEMBL4162545 162160 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc(F)c21 10.1021/acs.jmedchem.8b00322
156010733 177056 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633062 177056 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156013130 177478 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639514 177478 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156016840 177607 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 621 7 3 7 3.4 Cc1nc(-c2cccc(C(F)(F)F)c2)sc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
CHEMBL4641215 177607 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 621 7 3 7 3.4 Cc1nc(-c2cccc(C(F)(F)F)c2)sc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1 10.1021/acs.jmedchem.0c00828
156021942 178199 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4649860 178199 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44570920 183909 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 413 4 1 4 2.5 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
CHEMBL481408 183909 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 413 4 1 4 2.5 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccccc3)cc2)C1 10.1016/j.bmcl.2008.12.042
44571005 184023 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 431 4 1 5 2.6 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CCCNCC3)cc2)o1 10.1016/j.bmcl.2008.12.042
CHEMBL482204 184023 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
ChEMBL 431 4 1 5 2.6 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CCCNCC3)cc2)o1 10.1016/j.bmcl.2008.12.042
11539144 88864 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 425 5 2 5 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2ccccc2c1 10.6019/CHEMBL2364335
CHEMBL2364356 88864 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 425 5 2 5 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2ccccc2c1 10.6019/CHEMBL2364335
69197315 88880 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1cc(F)c(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
CHEMBL2364372 88880 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 475 6 2 6 4.6 COc1cc(F)c(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1 10.6019/CHEMBL2364335
11683663 88906 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccoc2)cc1 10.6019/CHEMBL2364335
CHEMBL2364398 88906 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccoc2)cc1 10.6019/CHEMBL2364335
11583902 88947 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 484 6 2 6 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)cc1F 10.6019/CHEMBL2364335
CHEMBL2364437 88947 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 484 6 2 6 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)cc1F 10.6019/CHEMBL2364335
69198030 88952 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 479 5 2 5 5.2 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)cc3Cl)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
CHEMBL2364442 88952 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 479 5 2 5 5.2 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)cc3Cl)c2)C[C@@H](C)N1 10.6019/CHEMBL2364335
69197149 88964 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)c(C)c1 10.6019/CHEMBL2364335
CHEMBL2364454 88964 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)c(C)c1 10.6019/CHEMBL2364335
69196669 88989 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 456 6 2 7 3.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)nc1 10.6019/CHEMBL2364335
CHEMBL2364478 88989 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 456 6 2 7 3.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)nc1 10.6019/CHEMBL2364335
10032659 12019 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 587 11 4 8 -0.5 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@H](CO)NC(=O)CN)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL1183505 12019 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 587 11 4 8 -0.5 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@H](CO)NC(=O)CN)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL301259 12019 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL 587 11 4 8 -0.5 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@H](CO)NC(=O)CN)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
44450137 96272 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 465 12 3 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)Nc1ccccc1 10.1016/j.bmcl.2008.03.059
CHEMBL261234 96272 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 465 12 3 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)Nc1ccccc1 10.1016/j.bmcl.2008.03.059
127046472 139669 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1021/acs.jmedchem.1c02191
CHEMBL3798056 139669 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1021/acs.jmedchem.1c02191
127046472 139669 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayInverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798056 139669 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayInverse agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
145988286 167182 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 542 6 1 6 5.4 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-n5nccn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4291718 167182 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 542 6 1 6 5.4 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-n5nccn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL3578007 211738 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm501702q
CHEMBL61663 215816 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1aFunctional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/s0960-894x(01)00324-9
24180592 96984 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
CHEMBL266647 96984 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
162663868 181964 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 672 14 3 9 3.8 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4780408 181964 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 672 14 3 9 3.8 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
145986080 166428 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 489 5 1 3 6.2 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(C)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4277793 166428 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 489 5 1 3 6.2 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(C)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
168274297 190555 0 None - 1 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 299 6 1 1 5.3 CCCCCCCc1cc(=O)c2cc(C(C)(C)C)ccc2[nH]1 10.1021/acs.jmedchem.1c02191
CHEMBL5180310 190555 0 None - 1 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 299 6 1 1 5.3 CCCCCCCc1cc(=O)c2cc(C(C)(C)C)ccc2[nH]1 10.1021/acs.jmedchem.1c02191
127047523 140038 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 859 20 7 9 6.0 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3800422 140038 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 859 20 7 9 6.0 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)O)cc1 10.1016/j.bmcl.2016.04.003
44434118 148154 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 467 14 3 9 0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCCNS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL393570 148154 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 467 14 3 9 0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCCNS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
44446187 94592 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252255 94592 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
145959787 162261 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 162261 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
155557019 174563 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4556887 174563 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
56926893 69034 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 10.1021/jm2007062
CHEMBL1923637 69034 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 10.1021/jm2007062
44437963 202069 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 452 6 1 3 4.5 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c(Br)cccc21 10.1016/j.bmc.2007.01.057
CHEMBL608826 202069 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 452 6 1 3 4.5 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c(Br)cccc21 10.1016/j.bmc.2007.01.057
44437963 202069 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 452 6 1 3 4.5 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c(Br)cccc21 10.1016/j.bmc.2007.01.057
CHEMBL608826 202069 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 452 6 1 3 4.5 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c(Br)cccc21 10.1016/j.bmc.2007.01.057
44579881 186812 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1ccccc1Cl 10.1016/j.bmcl.2008.07.120
CHEMBL489402 186812 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 392 6 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1ccccc1Cl 10.1016/j.bmcl.2008.07.120
24180646 148158 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1021/jm701137s
CHEMBL393576 148158 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1021/jm701137s
24180646 148158 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
CHEMBL393576 148158 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1016/j.bmcl.2007.07.097
145959787 162261 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 162261 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
46882520 5824 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 430 5 2 4 3.8 Cc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1Cl 10.1016/j.bmcl.2009.09.027
CHEMBL1079311 5824 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 430 5 2 4 3.8 Cc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1Cl 10.1016/j.bmcl.2009.09.027
46882458 5946 0 None -31 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 438 8 2 4 4.2 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL1080046 5946 0 None -31 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
ChEMBL 438 8 2 4 4.2 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1 10.1016/j.bmcl.2009.09.027
CHEMBL3578016 211744 0 None -15 2 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
59007057 88863 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 6 2.8 COc1ccc(NS(=O)(=O)c2ccc(N3CCCC3=O)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364355 88863 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 458 6 2 6 2.8 COc1ccc(NS(=O)(=O)c2ccc(N3CCCC3=O)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
11597905 88917 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 6 2 5 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(C)cc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
CHEMBL2364409 88917 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 465 6 2 5 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(C)cc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1 10.6019/CHEMBL2364335
69198135 88948 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 484 6 2 6 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)c(F)c1 10.6019/CHEMBL2364335
CHEMBL2364438 88948 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 484 6 2 6 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)c(F)c1 10.6019/CHEMBL2364335
11711997 88965 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 446 5 2 7 2.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2c(c1)OCCN2C 10.6019/CHEMBL2364335
CHEMBL2364455 88965 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
ChEMBL 446 5 2 7 2.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2c(c1)OCCN2C 10.6019/CHEMBL2364335
44452778 159754 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 499 6 2 7 3.5 C[C@H]1CN(c2ccc(C(=O)N(C)C)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
CHEMBL410527 159754 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
ChEMBL 499 6 2 7 3.5 C[C@H]1CN(c2ccc(C(=O)N(C)C)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1 10.1016/j.bmcl.2007.12.021
10437444 112854 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 546 11 2 4 3.8 CNC(=O)[C@@H](Cc1ccc(F)cc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL330989 112854 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 546 11 2 4 3.8 CNC(=O)[C@@H](Cc1ccc(F)cc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
24969603 69025 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 520 3 3 5 2.4 Cc1ccc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NCCOc3ccccc3CCCNC2=O)cc1 10.1021/jm2007062
CHEMBL1923627 69025 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 520 3 3 5 2.4 Cc1ccc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NCCOc3ccccc3CCCNC2=O)cc1 10.1021/jm2007062
162649450 180030 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 725 14 3 10 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C2CCN(c3oc(C)nc3C#N)CC2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4747770 180030 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 725 14 3 10 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C2CCN(c3oc(C)nc3C#N)CC2)cc1 10.1021/acs.jmedchem.9b02122
156013130 177478 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639514 177478 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44450100 160631 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 511 14 4 10 0.6 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1cccc(C(=O)NCCO)c1 10.1016/j.bmcl.2008.03.059
CHEMBL411330 160631 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
ChEMBL 511 14 4 10 0.6 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1cccc(C(=O)NCCO)c1 10.1016/j.bmcl.2008.03.059
44411720 10275 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161826 10275 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
44411902 10279 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161831 10279 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
44411720 10275 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161826 10275 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1016/j.bmc.2007.01.057
44411902 10279 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
CHEMBL1161831 10279 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1016/j.bmc.2007.01.057
162656896 180836 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 669 14 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2cccs2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4757313 180836 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 669 14 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2cccs2)cc1 10.1021/acs.jmedchem.9b02122
44436883 146128 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 604 11 6 7 3.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2c[nH]c3ccccc23)cc1 10.1021/jm0704550
CHEMBL391980 146128 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 604 11 6 7 3.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2c[nH]c3ccccc23)cc1 10.1021/jm0704550
156010733 177056 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633062 177056 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
10745674 167930 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 572 13 3 5 3.5 C[C@@H](O)CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL431668 167930 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 572 13 3 5 3.5 C[C@@H](O)CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
44579776 193227 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 352 7 1 3 3.5 Cc1cccc(CN(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
CHEMBL523795 193227 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 352 7 1 3 3.5 Cc1cccc(CN(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1 10.1016/j.bmcl.2008.07.120
127048061 139711 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 903 24 7 11 5.9 COC(=O)[C@H](CC(C)C)NC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798337 139711 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assayAgonist activity at human GHS-R1a expressed in HEK293T cells after 45 mins by HTRF-based IP3 turnover assay
ChEMBL 903 24 7 11 5.9 COC(=O)[C@H](CC(C)C)NC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
23730340 89712 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 504 15 4 10 0.4 CC(=O)NCCCCNC(=O)OCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1021/jm7010595
CHEMBL237700 89712 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 504 15 4 10 0.4 CC(=O)NCCCCNC(=O)OCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1021/jm7010595
56926175 68984 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923504 68984 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
145992835 166810 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cncnc4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4285075 166810 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cncnc4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
56925343 69037 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 550 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cccc3c2O[C@H](CC3)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923640 69037 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assayAgonist activity at human GRLN receptor expressed in HEK293 cells assessed as calcium binding by Ca2+ bioluminescence aequorin assay
ChEMBL 550 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cccc3c2O[C@H](CC3)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
145986870 167116 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 505 6 1 4 5.9 COc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(OC)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4290627 167116 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 505 6 1 4 5.9 COc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(OC)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
44434054 89275 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2cccc(NS(C)(=O)=O)c2)n1 10.1016/j.bmcl.2007.07.099
CHEMBL236857 89275 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2cccc(NS(C)(=O)=O)c2)n1 10.1016/j.bmcl.2007.07.099
44446178 155099 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL402023 155099 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilizationAgonist activity at human GHSR1a receptor expressed in CHO cells assessed as intracellular calcium mobilization
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL3578016 211744 0 None -15 2 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
162648837 179814 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 706 15 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4745116 179814 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293 cells assessed as inhibition of ghrelin-induced IP1 response measured after 30 mins by HTRF assay
ChEMBL 706 15 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
44391024 64255 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 527 11 1 4 5.2 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)Cc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180992 64255 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 527 11 1 4 5.2 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)Cc1ccccc1)C(C)C 10.1016/j.bmcl.2005.02.040
10745674 167930 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 572 13 3 5 3.5 C[C@@H](O)CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
CHEMBL431668 167930 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
ChEMBL 572 13 3 5 3.5 C[C@@H](O)CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm980197u
44391021 19421 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 569 12 1 5 5.3 CC(=O)C(C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C)c1ccccc1 10.1016/j.bmcl.2005.02.040
CHEMBL129637 19421 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 569 12 1 5 5.3 CC(=O)C(C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C)c1ccccc1 10.1016/j.bmcl.2005.02.040
CHEMBL2170696 209333 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1csc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1csc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
23730343 89874 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 475 12 3 10 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NC[C@H]1CCCO1 10.1021/jm7010595
CHEMBL237917 89874 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assayIntrinsic activity at human GHS receptor in H4 glioma cells assessed by measuring intracellular calcium concentration by FLIPR assay
ChEMBL 475 12 3 10 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NC[C@H]1CCCO1 10.1021/jm7010595
22888359 63886 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 520 10 1 6 4.8 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C#N)C(C)C 10.1016/j.bmcl.2005.02.040
CHEMBL180591 63886 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
ChEMBL 520 10 1 6 4.8 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C#N)C(C)C 10.1016/j.bmcl.2005.02.040
16114514 79129 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCCNC1 10.1021/jm0704550
CHEMBL2113322 79129 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium levelAgonist activity at human GHS1a receptor expressed in CHO cells assessed as accumulation of intracellular calcium level
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCCNC1 10.1021/jm0704550
44579843 184729 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL485092 184729 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 358 6 1 3 3.9 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
44579643 186747 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 338 7 1 3 3.2 CC(Oc1ccccc1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL488971 186747 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 338 7 1 3 3.2 CC(Oc1ccccc1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44579822 192500 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1cccc(CN(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL520953 192500 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 386 7 1 3 4.2 Cc1cccc(CN(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2Cl)c1 10.1016/j.bmcl.2008.07.120
44579755 186919 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 352 8 1 3 3.6 CCC(Oc1ccccc1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL490186 186919 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 352 8 1 3 3.6 CCC(Oc1ccccc1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
44580032 186810 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 363 7 1 4 3.3 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(CC#N)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL489398 186810 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at GHSRAgonist activity at GHSR
ChEMBL 363 7 1 4 3.3 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(CC#N)cc1 10.1016/j.bmcl.2008.07.120
145991945 166791 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 615 6 1 4 7.8 CCN(C(=O)N[C@@H](C)c1ccc(C#CC2CC2)c(Cl)c1Cl)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4284715 166791 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 615 6 1 4 7.8 CCN(C(=O)N[C@@H](C)c1ccc(C#CC2CC2)c(Cl)c1Cl)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1 10.1021/acs.jmedchem.8b00794
145992253 166904 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 595 6 1 6 6.4 COC(=O)c1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4286849 166904 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 595 6 1 6 6.4 COC(=O)c1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL2170702 209339 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
145993313 166868 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 577 7 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3cccc(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4286101 166868 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Inverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assayInverse agonist at recombinant human GHSR1a expressed in HEK293 cells assessed as decrease in IP1 accumulation after 1 hr by IP1-d2-based HTRF assay
ChEMBL 577 7 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3cccc(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
16114008 84817 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 536 11 3 6 4.7 COc1ccccc1Cn1c(CCc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL223532 84817 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilizationAgonist activity at human GHS1a receptor expressed in CHO cells assessed as induction of intracellular calcium mobilization
ChEMBL 536 11 3 6 4.7 COc1ccccc1Cn1c(CCc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL501261 214112 23 None - 1 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assayInverse agonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in inositol phosphate production after 30 mins by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.8b01644
9848305 145427 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccc(NS(C)(=O)=O)cc2)n1 10.1016/j.bmcl.2007.07.099
CHEMBL391429 145427 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccc(NS(C)(=O)=O)cc2)n1 10.1016/j.bmcl.2007.07.099
44434050 145425 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL391428 145425 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL3578015 211743 0 None -33 2 Human 7.0 pEC50 = 7 Functional
Inverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatographyInverse agonist activity at human GHSR1a receptor expressed in COS-7 cells assessed as inositol phosphate accumulation after 2 hrs by anion exchange chromatography
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
CHEMBL369482 212140 0 None - 0 Rat 8.0 pED50 = 8 Functional
In vitro effective dose was measured for the growth hormone release in rat pituitary cellsIn vitro effective dose was measured for the growth hormone release in rat pituitary cells
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cn1ccnc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/S0960-894X(01)80239-0
44269087 98199 0 None - 1 Rat 6.7 pED50 = 6.7 Functional
In vitro effective dose was measured for the growth hormone release in rat pituitary cellsIn vitro effective dose was measured for the growth hormone release in rat pituitary cells
ChEMBL 553 10 4 7 3.2 CC(C)(NCCCO)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=O 10.1016/S0960-894X(01)80239-0
CHEMBL274341 98199 0 None - 1 Rat 6.7 pED50 = 6.7 Functional
In vitro effective dose was measured for the growth hormone release in rat pituitary cellsIn vitro effective dose was measured for the growth hormone release in rat pituitary cells
ChEMBL 553 10 4 7 3.2 CC(C)(NCCCO)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=O 10.1016/S0960-894X(01)80239-0
70691550 73171 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 572 8 2 5 5.1 Cc1cc(F)ccc1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
CHEMBL2011825 73171 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 572 8 2 5 5.1 Cc1cc(F)ccc1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
16114292 96905 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL266063 96905 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL509976 215557 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Agonist activity at human ghrelin receptor Met5:05Ala(Met213) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Met5:05Ala(Met213) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
25260901 113453 1 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL 577 5 2 9 3.6 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/acs.jmedchem.1c02191
CHEMBL3319405 113453 1 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL 577 5 2 9 3.6 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/acs.jmedchem.1c02191
71456897 81821 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 513 5 2 3 5.7 CCN1CCC(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164507 81821 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 513 5 2 3 5.7 CCN1CCC(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
70691551 73172 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 568 8 2 5 5.3 Cc1cccc(C)c1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
CHEMBL2011826 73172 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 568 8 2 5 5.3 Cc1cccc(C)c1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
25261382 113414 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Partial agonist activity at GHS-R1a (unknown origin)Partial agonist activity at GHS-R1a (unknown origin)
ChEMBL 535 7 2 8 3.3 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/acs.jmedchem.1c02191
CHEMBL3319215 113414 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Partial agonist activity at GHS-R1a (unknown origin)Partial agonist activity at GHS-R1a (unknown origin)
ChEMBL 535 7 2 8 3.3 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/acs.jmedchem.1c02191
11431274 77315 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 467 9 3 8 3.8 CC(C)=CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL208424 77315 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 467 9 3 8 3.8 CC(C)=CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11577349 65201 1 None - 1 Human 8.0 pIC50 = 8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 529 9 1 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCN(C)C2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL182655 65201 1 None - 1 Human 8.0 pIC50 = 8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 529 9 1 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCN(C)C2=O)cc1 10.1016/j.bmcl.2004.06.060
11351838 77621 0 None - 1 Human 8.0 pIC50 = 8 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 468 8 4 6 4.9 CC(NC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1)c1ccccc1 10.1021/jm060461g
CHEMBL208842 77621 0 None - 1 Human 8.0 pIC50 = 8 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 468 8 4 6 4.9 CC(NC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1)c1ccccc1 10.1021/jm060461g
11712151 75964 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 453 9 3 7 4.8 CC(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL205470 75964 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 453 9 3 7 4.8 CC(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
11713497 123211 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 531 9 1 6 6.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)c(C)c1 10.1016/j.bmcl.2004.11.075
CHEMBL361349 123211 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 531 9 1 6 6.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)c(C)c1 10.1016/j.bmcl.2004.11.075
44409757 141299 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 506 8 3 8 4.1 CN(Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL383454 141299 0 None - 1 Human 8.0 pIC50 = 8 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 506 8 3 8 4.1 CN(Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1)c1ccc(F)cc1 10.1016/j.bmcl.2006.01.012
127046807 139915 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799671 139915 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
3676358 5502 4 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 409 3 1 2 4.4 O=C(c1ccc(-c2ccccc2)cc1)N1CCN(C(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/j.bmcl.2010.01.043
CHEMBL1076586 5502 4 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 409 3 1 2 4.4 O=C(c1ccc(-c2ccccc2)cc1)N1CCN(C(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/j.bmcl.2010.01.043
122182047 121976 0 None -67 2 Rat 7.0 pIC50 = 7 Functional
Antagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assayAntagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assay
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593636 121976 0 None -67 2 Rat 7.0 pIC50 = 7 Functional
Antagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assayAntagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assay
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
122178603 121313 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 590 11 2 6 6.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(Cl)nc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581036 121313 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 590 11 2 6 6.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(Cl)nc2)cc1 10.1016/j.bmcl.2014.11.031
11649248 66640 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 515 9 1 5 7.2 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL185399 66640 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 515 9 1 5 7.2 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCCO2)cc1 10.1016/j.bmcl.2004.06.060
44395020 124006 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 507 9 1 5 6.1 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL363021 124006 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 507 9 1 5 6.1 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)CC1 10.1016/j.bmcl.2004.06.060
44389262 122006 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 479 6 2 4 6.1 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccccc1 10.1016/j.bmcl.2004.11.075
CHEMBL359506 122006 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 479 6 2 4 6.1 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccccc1 10.1016/j.bmcl.2004.11.075
145993628 167367 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 483 4 1 2 6.1 C#Cc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(C)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4295148 167367 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 483 4 1 2 6.1 C#Cc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(C)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
11211892 80187 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 405 8 3 6 4.0 CC(C)CC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
CHEMBL213703 80187 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 405 8 3 6 4.0 CC(C)CC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
122178611 121322 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 572 11 3 7 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2O)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581044 121322 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 572 11 3 7 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2O)cc1 10.1016/j.bmcl.2014.11.031
11846624 77887 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 490 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(C1CCCC1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
CHEMBL209443 77887 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 490 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(C1CCCC1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
11846463 139217 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 422 5 2 8 2.7 CCc1nc(N)nc(N)c1-c1ccc2c(c1)ncn2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
CHEMBL378909 139217 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 422 5 2 8 2.7 CCc1nc(N)nc(N)c1-c1ccc2c(c1)ncn2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
11430392 76695 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 431 6 3 7 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Cl)c1 10.1021/jm0510934
CHEMBL206588 76695 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 431 6 3 7 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Cl)c1 10.1021/jm0510934
57797614 73163 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 558 8 2 5 4.8 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(F)cc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011817 73163 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 558 8 2 5 4.8 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(F)cc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
44409801 76704 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 5 3 7 3.6 CC(C)(C)c1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206638 76704 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 5 3 7 3.6 CC(C)(C)c1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11523411 75526 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 363 6 4 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)O)cc2)cc1 10.1021/jm0510934
CHEMBL204511 75526 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 363 6 4 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)O)cc2)cc1 10.1021/jm0510934
11537800 75538 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 361 6 3 6 3.7 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)=O)cc2)cc1 10.1021/jm0510934
CHEMBL204564 75538 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 361 6 3 6 3.7 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)=O)cc2)cc1 10.1021/jm0510934
71453392 81818 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 5 2 4 4.2 CN(C)[C@H]1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)C1 10.1016/j.bmc.2012.07.018
CHEMBL2164504 81818 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 5 2 4 4.2 CN(C)[C@H]1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)C1 10.1016/j.bmc.2012.07.018
71456910 81872 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 480 5 2 4 3.6 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164823 81872 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 480 5 2 4 3.6 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
71460578 81879 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)ccc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164830 81879 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)ccc32)CC1 10.1016/j.bmc.2012.07.018
122178612 121323 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 572 11 2 6 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc[n+]2[O-])cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581045 121323 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 572 11 2 6 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc[n+]2[O-])cc1 10.1016/j.bmcl.2014.11.031
CHEMBL507636 214410 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H]1CCCN1C(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1074/jbc.m609796200
56942387 139637 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 579 13 4 7 4.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797857 139637 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 579 13 4 7 4.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
145991822 166935 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 6.8 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)NCc3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4287267 166935 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 6.8 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)NCc3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
11676995 66132 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 461 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCOC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL184258 66132 1 None - 1 Human 6.9 pIC50 = 6.9 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 461 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCOC)cc1 10.1016/j.bmcl.2004.06.060
127048038 139947 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 551 11 4 7 4.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799862 139947 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 551 11 4 7 4.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
71458746 81808 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1ccc2c(c1Cl)C(NC(=O)CN1CCN(C)CC1)(c1ccc(Cl)cc1)C(=O)N2 10.1016/j.bmc.2012.07.018
CHEMBL2164493 81808 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1ccc2c(c1Cl)C(NC(=O)CN1CCN(C)CC1)(c1ccc(Cl)cc1)C(=O)N2 10.1016/j.bmc.2012.07.018
145992142 166747 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 475 4 2 3 5.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(O)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4283858 166747 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 475 4 2 3 5.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(O)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
71460565 81810 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1cccc(Cl)c1 10.1016/j.bmc.2012.07.018
CHEMBL2164495 81810 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1cccc(Cl)c1 10.1016/j.bmc.2012.07.018
11538533 74972 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
CHEMBL203280 74972 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
46880462 6235 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)[C@@H](C)C3)cc2)c1 10.1016/j.bmcl.2010.01.043
CHEMBL1081648 6235 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)[C@@H](C)C3)cc2)c1 10.1016/j.bmcl.2010.01.043
70693641 73174 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 538 8 2 5 4.4 O=C1CN([C@@H](C(=O)NC2CCN(Cc3ccccc3)CC2)C2CC2)C(=O)c2cc(Oc3ccccc3)ccc2N1 10.1016/j.bmcl.2012.01.014
CHEMBL2011828 73174 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 538 8 2 5 4.4 O=C1CN([C@@H](C(=O)NC2CCN(Cc3ccccc3)CC2)C2CC2)C(=O)c2cc(Oc3ccccc3)ccc2N1 10.1016/j.bmcl.2012.01.014
44409756 76738 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 492 8 4 8 4.1 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccc(F)cc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206820 76738 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 492 8 4 8 4.1 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccc(F)cc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
46865987 7565 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 442 3 1 3 4.4 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3)c(F)c2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1087908 7565 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 442 3 1 3 4.4 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3)c(F)c2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
46880772 5879 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1079624 5879 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
11538534 74985 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
CHEMBL203373 74985 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
145986870 167116 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 505 6 1 4 5.9 COc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(OC)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4290627 167116 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 505 6 1 4 5.9 COc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(OC)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
127046806 139908 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 638 13 4 7 5.4 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799604 139908 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 638 13 4 7 5.4 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
122178613 121324 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 625 12 2 7 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(N3CCCC3)cn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581046 121324 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 625 12 2 7 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(N3CCCC3)cn2)cc1 10.1016/j.bmcl.2014.11.031
145981196 166512 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 627 5 1 6 7.1 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)N[C@@H](C)c4ccc(-c5cnccn5)c(Cl)c4Cl)CC3)C2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4279344 166512 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 627 5 1 6 7.1 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)N[C@@H](C)c4ccc(-c5cnccn5)c(Cl)c4Cl)CC3)C2)ncn1 10.1021/acs.jmedchem.8b00794
46880814 6345 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 413 3 2 3 3.5 C[C@H]1CN(C(=O)c2ccc(-c3cn[nH]c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1082190 6345 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 413 3 2 3 3.5 C[C@H]1CN(C(=O)c2ccc(-c3cn[nH]c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
122178616 121326 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc3ccccc3cn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581048 121326 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc3ccccc3cn2)cc1 10.1016/j.bmcl.2014.11.031
145986461 167189 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4291926 167189 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
71451551 81822 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 460 5 2 4 3.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(C)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164508 81822 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 460 5 2 4 3.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(C)cc32)CC1 10.1016/j.bmc.2012.07.018
46880727 6113 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 458 3 1 3 4.9 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3Cl)nc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080939 6113 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 458 3 1 3 4.9 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3Cl)nc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
122182190 121983 0 None -8 2 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assayAntagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assay
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
CHEMBL3593815 121983 0 None -8 2 Rat 7.9 pIC50 = 7.9 Functional
Antagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assayAntagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assay
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
44409840 76313 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 500 7 3 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN3CCc4ccccc43)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205896 76313 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 500 7 3 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN3CCc4ccccc43)cc2)cc1 10.1016/j.bmcl.2006.01.012
127047362 139694 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 590 11 5 7 4.7 COc1ccc(Cn2c([C@H](N)Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798204 139694 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 590 11 5 7 4.7 COc1ccc(Cn2c([C@H](N)Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
145989916 166722 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 491 5 2 4 5.6 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(O)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4283454 166722 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 491 5 2 4 5.6 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(O)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
127048038 139947 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 551 11 4 7 4.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799862 139947 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 551 11 4 7 4.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
46880673 6073 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 507 4 1 3 5.7 C[C@H]1CN(C(=O)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080755 6073 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 507 4 1 3 5.7 C[C@H]1CN(C(=O)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
11455251 161290 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 523 8 3 7 5.0 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3Br)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL412362 161290 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 523 8 3 7 5.0 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3Br)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
44409611 74658 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 463 6 3 7 4.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CC4CCC3C4)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203019 74658 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 463 6 3 7 4.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CC4CCC3C4)cc2)cc1 10.1016/j.bmcl.2006.01.012
11221946 140821 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm0510934
CHEMBL381942 140821 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm0510934
44409839 76229 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 412 7 4 8 2.0 CNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205847 76229 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 412 7 4 8 2.0 CNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
71460576 81876 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3c(Cl)cc(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164828 81876 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3c(Cl)cc(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL509976 215557 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Agonist activity at human ghrelin receptor Ser5:09Ala(Ser217) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Ser5:09Ala(Ser217) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
11692087 62962 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178610 62962 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.11.075
44409758 75945 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 411 6 3 7 3.4 CC(C)c1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205374 75945 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 411 6 3 7 3.4 CC(C)c1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409661 75967 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 423 6 3 7 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205484 75967 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 423 6 3 7 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
46880724 6226 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 437 3 1 2 5.1 Cc1cc(-c2ccccc2)ccc1C(=O)N1CCN(C(=O)c2ccc3cc[nH]c3c2)[C@@H](C)C1 10.1016/j.bmcl.2010.01.043
CHEMBL1081611 6226 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 437 3 1 2 5.1 Cc1cc(-c2ccccc2)ccc1C(=O)N1CCN(C(=O)c2ccc3cc[nH]c3c2)[C@@H](C)C1 10.1016/j.bmcl.2010.01.043
71455105 81875 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 432 4 2 4 2.6 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)ccc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164827 81875 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 432 4 2 4 2.6 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)ccc32)CC1 10.1016/j.bmc.2012.07.018
11221946 140821 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm060461g
CHEMBL381942 140821 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm060461g
44410003 76152 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 468 10 4 8 3.5 CC(C)CCNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205794 76152 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 468 10 4 8 3.5 CC(C)CCNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
46880811 5966 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3cccnc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080162 5966 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3cccnc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
70687379 73169 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 570 9 2 6 4.7 COc1cccc(Oc2ccc3c(c2)C(=O)N([C@@H](C(=O)NC2CCN(Cc4ccccc4)CC2)C(C)C)CC(=O)N3)c1 10.1016/j.bmcl.2012.01.014
CHEMBL2011823 73169 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 570 9 2 6 4.7 COc1cccc(Oc2ccc3c(c2)C(=O)N([C@@H](C(=O)NC2CCN(Cc4ccccc4)CC2)C(C)C)CC(=O)N3)c1 10.1016/j.bmcl.2012.01.014
44394974 66982 1 None - 1 Human 6.8 pIC50 = 6.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 515 9 1 5 7.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCOCC2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL186974 66982 1 None - 1 Human 6.8 pIC50 = 6.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 515 9 1 5 7.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCOCC2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL3586019 211778 6 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by inositol phosphate turnover assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by inositol phosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CCCNC(=N)N)C(N)=O 10.1016/j.bmcl.2015.04.040
46880567 6355 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3cccc(F)c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1082210 6355 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3cccc(F)c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
71460564 81807 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 488 4 2 4 3.9 CN1CCN(CC(=O)NC2(c3ccc(C(C)(C)C)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164492 81807 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 488 4 2 4 3.9 CN1CCN(CC(=O)NC2(c3ccc(C(C)(C)C)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
145992854 166842 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 7.0 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)C2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4285747 166842 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 7.0 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)C2)ncn1 10.1021/acs.jmedchem.8b00794
44394833 126799 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 542 9 1 5 6.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2C(=O)CCC2(C)C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL365460 126799 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 542 9 1 5 6.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2C(=O)CCC2(C)C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL509976 215557 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Agonist activity at human ghrelin receptor Asn7:02Ala(Asn305) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Asn7:02Ala(Asn305) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
CHEMBL509976 215557 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Agonist activity at human wild type ghrelin receptor expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human wild type ghrelin receptor expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
CHEMBL509976 215557 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
127047654 139952 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799883 139952 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
145993758 167292 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 490 5 2 4 5.4 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(N)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4294024 167292 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 490 5 2 4 5.4 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(N)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
145993528 167294 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 561 5 1 4 6.6 C#Cc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4294083 167294 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 561 5 1 4 6.6 C#Cc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL444131 213906 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None NC(=O)CNC(=O)CNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1c[nH]c2ccccc12 10.1074/jbc.m609796200
11476589 75959 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(CNc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205451 75959 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(CNc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
11329138 64430 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilizationAntagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilization
ChEMBL 481 9 1 5 5.1 CCN(CC)c1ccc(NC(=O)C2(N(C)C(=O)OCC(C)C)CCc3cccc(OC)c3C2)cc1 10.1016/j.bmcl.2012.01.014
CHEMBL181350 64430 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilizationAntagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilization
ChEMBL 481 9 1 5 5.1 CCN(CC)c1ccc(NC(=O)C2(N(C)C(=O)OCC(C)C)CCc3cccc(OC)c3C2)cc1 10.1016/j.bmcl.2012.01.014
70681022 73178 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 568 8 2 5 5.4 CC(C)[C@H](C(=O)N1CCC(NC(C)(C)c2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011833 73178 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 568 8 2 5 5.4 CC(C)[C@H](C(=O)N1CCC(NC(C)(C)c2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL509976 215557 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human ghrelin receptor Ile4:20Ala(Ile178) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Ile4:20Ala(Ile178) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
122178611 121322 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 572 11 3 7 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2O)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581044 121322 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 572 11 3 7 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2O)cc1 10.1016/j.bmcl.2014.11.031
46880675 6111 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3)cc2F)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080927 6111 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3)cc2F)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
11612155 140984 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3csc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL382375 140984 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3csc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
328912 62546 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 505 5 1 4 7.0 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1CC1c2ccccc2CCN1C 10.1016/j.bmcl.2004.11.075
CHEMBL178266 62546 1 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 505 5 1 4 7.0 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1CC1c2ccccc2CCN1C 10.1016/j.bmcl.2004.11.075
70685218 73166 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 574 8 2 5 5.3 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3cccc(Cl)c3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011820 73166 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 574 8 2 5 5.3 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3cccc(Cl)c3)cc2C1=O 10.1016/j.bmcl.2012.01.014
145981794 166672 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 567 6 1 5 6.6 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4282394 166672 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 567 6 1 5 6.6 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
11649239 66310 1 None - 1 Human 7.8 pIC50 = 7.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 514 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL185057 66310 1 None - 1 Human 7.8 pIC50 = 7.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 514 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL501261 214112 23 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)CCCNC(=N)N)C(N)=O 10.1074/jbc.m609796200
1744826 62968 17 None - 1 Human 6.8 pIC50 = 6.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL178668 62968 17 None - 1 Human 6.8 pIC50 = 6.8 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.06.060
11282247 165902 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL425048 165902 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
11282247 165902 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL425048 165902 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
1744826 62968 17 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178668 62968 17 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44409831 75669 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 503 6 3 9 3.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3COc4ccccc4O3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204776 75669 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 503 6 3 9 3.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3COc4ccccc4O3)cc2)cc1 10.1016/j.bmcl.2006.01.012
145979268 166640 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 607 8 1 5 7.4 COc1ccc([C@H](CC2CC2)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4281647 166640 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 607 8 1 5 7.4 COc1ccc([C@H](CC2CC2)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
44409678 141192 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 490 9 3 9 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3cccnc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL382853 141192 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 490 9 3 9 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3cccnc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11349789 78744 1 None - 1 Human 6.7 pIC50 = 6.7 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 389 7 3 6 3.4 Nc1nc(N)c(-c2ccc(NC(=O)C3CC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL211265 78744 1 None - 1 Human 6.7 pIC50 = 6.7 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 389 7 3 6 3.4 Nc1nc(N)c(-c2ccc(NC(=O)C3CC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
11692087 62962 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL178610 62962 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.06.060
11677781 125032 1 None - 1 Human 7.7 pIC50 = 7.7 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 502 9 1 5 5.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN(C)C(C)=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL364430 125032 1 None - 1 Human 7.7 pIC50 = 7.7 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 502 9 1 5 5.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN(C)C(C)=O)cc1 10.1016/j.bmcl.2004.06.060
11538533 74972 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm060461g
CHEMBL203280 74972 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm060461g
11154823 76000 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 436 8 3 7 4.5 N#Cc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL205660 76000 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 436 8 3 7 4.5 N#Cc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
56942244 125171 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645259 125171 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
44409994 76153 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 409 6 3 7 3.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205796 76153 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 409 6 3 7 3.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44576247 214199 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inverse agonist activity at human ghrelin receptor Phe5:12Ala(Phe220) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Phe5:12Ala(Phe220) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 214199 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inverse agonist activity at human ghrelin receptor Phe5:12Ala(Phe220) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Phe5:12Ala(Phe220) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
44395002 66156 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 534 9 1 5 5.6 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL184368 66156 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 534 9 1 5 5.6 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)CC1 10.1016/j.bmcl.2004.06.060
11646276 75905 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
CHEMBL205136 75905 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
127046807 139915 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799671 139915 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
16113695 137002 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL374643 137002 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
145987684 167253 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 615 6 1 4 7.8 CC[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4293331 167253 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 615 6 1 4 7.8 CC[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
122178602 121312 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2Br)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581035 121312 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2Br)cc1 10.1016/j.bmcl.2014.11.031
70681020 73175 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011829 73175 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
56942098 125167 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645255 125167 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
56942242 125169 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645257 125169 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 10.1016/j.bmcl.2016.04.003
127046956 139932 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 631 12 3 7 5.5 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799776 139932 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 631 12 3 7 5.5 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2016.04.003
66788278 125166 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645254 125166 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
127046956 139932 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 631 12 3 7 5.5 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799776 139932 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 631 12 3 7 5.5 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2016.04.003
57797640 73197 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 510 9 1 3 7.1 CC(C)[C@H](C[C@H]1CC[C@@H](NCC2CC2)CC1)N1CCCc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011892 73197 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 510 9 1 3 7.1 CC(C)[C@H](C[C@H]1CC[C@@H](NCC2CC2)CC1)N1CCCc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
46880628 6000 0 None 4 2 Rat 8.7 pIC50 = 8.7 Functional
Inhibition of rat GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayInhibition of rat GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080389 6000 0 None 4 2 Rat 8.7 pIC50 = 8.7 Functional
Inhibition of rat GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayInhibition of rat GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
122178606 121316 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(F)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581039 121316 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(F)n2)cc1 10.1016/j.bmcl.2014.11.031
46880629 6026 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 457 3 1 2 5.5 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3Cl)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080556 6026 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 457 3 1 2 5.5 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3Cl)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
122178606 121316 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(F)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581039 121316 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(F)n2)cc1 10.1016/j.bmcl.2014.11.031
70681021 73177 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 554 8 2 5 5.2 CC(C)[C@H](C(=O)N1CCC(N[C@H](C)c2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011832 73177 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 554 8 2 5 5.2 CC(C)[C@H](C(=O)N1CCC(N[C@H](C)c2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
70691552 73179 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 560 8 2 5 5.4 CC(C)[C@H](C(=O)N1CCC(N[C@H](C)C2CCCCC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011834 73179 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 560 8 2 5 5.4 CC(C)[C@H](C(=O)N1CCC(N[C@H](C)C2CCCCC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
44576247 214199 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inverse agonist activity at human ghrelin receptor Ser4:16Ala(Ser174) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ser4:16Ala(Ser174) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 214199 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inverse agonist activity at human ghrelin receptor Ser4:16Ala(Ser174) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ser4:16Ala(Ser174) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
122178607 121318 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 592 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncc(F)cc2F)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581040 121318 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 592 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncc(F)cc2F)cc1 10.1016/j.bmcl.2014.11.031
46880631 6103 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 437 3 1 2 5.1 Cc1ccccc1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1 10.1016/j.bmcl.2010.01.043
CHEMBL1080907 6103 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 437 3 1 2 5.1 Cc1ccccc1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1 10.1016/j.bmcl.2010.01.043
46880726 6112 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3)nc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080938 6112 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3)nc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
70689441 73196 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 525 9 2 4 6.1 CC(C)[C@H](C[C@H]1CC[C@@H](NCC2CC2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011891 73196 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 525 9 2 4 6.1 CC(C)[C@H](C[C@H]1CC[C@@H](NCC2CC2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
145988582 167267 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 555 4 1 2 7.4 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C#C[Si](C)(C)C)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4293608 167267 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 555 4 1 2 7.4 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C#C[Si](C)(C)C)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
122178610 121321 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(N)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581043 121321 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(N)n2)cc1 10.1016/j.bmcl.2014.11.031
44409666 75858 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 437 6 3 7 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204897 75858 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 437 6 3 7 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44576247 214199 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inverse agonist activity at human ghrelin receptor Ser3:08Ala(Ser123) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ser3:08Ala(Ser123) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 214199 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inverse agonist activity at human ghrelin receptor Ser3:08Ala(Ser123) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ser3:08Ala(Ser123) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL500703 214097 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCNC(=N)N)C(N)=O 10.1074/jbc.m609796200
44409802 76715 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 9 3 7 4.1 CCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206687 76715 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 9 3 7 4.1 CCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122178613 121324 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 625 12 2 7 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(N3CCCC3)cn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581046 121324 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 625 12 2 7 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(N3CCCC3)cn2)cc1 10.1016/j.bmcl.2014.11.031
71458747 81809 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2012.07.018
CHEMBL2164494 81809 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2012.07.018
56942244 125171 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645259 125171 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
11537683 75498 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 354 5 3 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccnc(Cl)c2)cc1 10.1021/jm0510934
CHEMBL204352 75498 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 354 5 3 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccnc(Cl)c2)cc1 10.1021/jm0510934
71449740 81811 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 480 4 2 4 3.5 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2012.07.018
CHEMBL2164497 81811 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 480 4 2 4 3.5 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2012.07.018
122178601 121311 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cncc(Br)c2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581034 121311 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cncc(Br)c2)cc1 10.1016/j.bmcl.2014.11.031
11337482 76611 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
CHEMBL206399 76611 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
122178614 121325 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 660 13 2 7 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2C(=O)c2ccccc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581047 121325 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 660 13 2 7 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2C(=O)c2ccccc2)cc1 10.1016/j.bmcl.2014.11.031
44389168 64843 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 457 4 1 4 5.8 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCC1 10.1016/j.bmcl.2004.11.075
CHEMBL182154 64843 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 457 4 1 4 5.8 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCC1 10.1016/j.bmcl.2004.11.075
145991389 166980 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 6 1 6 6.5 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)NCc3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4288108 166980 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 6 1 6 6.5 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)NCc3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
145990051 166931 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 499 5 1 2 7.0 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C3CC3)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4287218 166931 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 499 5 1 2 7.0 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C3CC3)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
44410012 138374 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 9 3 7 4.1 CCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL377305 138374 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 9 3 7 4.1 CCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
71462272 81816 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 528 5 2 4 4.6 CN(C)C1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164502 81816 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 528 5 2 4 4.6 CN(C)C1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
71451563 81881 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 500 4 2 4 3.9 CN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164832 81881 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 500 4 2 4 3.9 CN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
145988286 167182 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 542 6 1 6 5.4 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-n5nccn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4291718 167182 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 542 6 1 6 5.4 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-n5nccn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
46880813 6344 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 442 3 1 4 4.4 Cc1noc(C)c1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1 10.1016/j.bmcl.2010.01.043
CHEMBL1082189 6344 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 442 3 1 4 4.4 Cc1noc(C)c1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1 10.1016/j.bmcl.2010.01.043
44409761 75837 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 9 3 7 4.4 CCc1nc(N)nc(NCC(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204880 75837 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 9 3 7 4.4 CCc1nc(N)nc(NCC(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11846625 77855 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 498 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(-c1ccccc1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
CHEMBL209394 77855 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 498 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(-c1ccccc1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
122178610 121321 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(N)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581043 121321 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(N)n2)cc1 10.1016/j.bmcl.2014.11.031
46880461 6203 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 439 4 1 3 4.4 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)CC3)cc2)c1 10.1016/j.bmcl.2010.01.043
CHEMBL1081483 6203 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 439 4 1 3 4.4 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)CC3)cc2)c1 10.1016/j.bmcl.2010.01.043
71453391 81817 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 5 2 4 4.2 CN(C)[C@@H]1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)C1 10.1016/j.bmc.2012.07.018
CHEMBL2164503 81817 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 5 2 4 4.2 CN(C)[C@@H]1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)C1 10.1016/j.bmc.2012.07.018
1221269 122008 12 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL359530 122008 12 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44389151 62475 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 445 6 1 4 5.7 CCN(CC)C(=O)c1ccccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
CHEMBL178138 62475 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 445 6 1 4 5.7 CCN(CC)C(=O)c1ccccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
71451564 81883 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)C(NC(=O)CN1CCN(C)CC1)(c1ccc(Cl)cc1)C(=O)N2 10.1016/j.bmc.2012.07.018
CHEMBL2164834 81883 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)C(NC(=O)CN1CCN(C)CC1)(c1ccc(Cl)cc1)C(=O)N2 10.1016/j.bmc.2012.07.018
71449753 81873 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 465 4 2 3 4.7 CC1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164825 81873 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 465 4 2 3 4.7 CC1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
44409871 75367 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 426 7 3 8 2.4 CN(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203948 75367 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 426 7 3 8 2.4 CN(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
46880569 6157 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1ccccc1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1 10.1016/j.bmcl.2010.01.043
CHEMBL1081212 6157 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1ccccc1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1 10.1016/j.bmcl.2010.01.043
70693640 73168 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 570 9 2 6 4.7 COc1ccccc1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
CHEMBL2011822 73168 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 570 9 2 6 4.7 COc1ccccc1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
CHEMBL449590 213939 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1074/jbc.m609796200
44576247 214199 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inverse agonist activity at human ghrelin receptor Val5:08Ala(Val216) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Val5:08Ala(Val216) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 214199 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inverse agonist activity at human ghrelin receptor Val5:08Ala(Val216) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Val5:08Ala(Val216) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
145994299 167372 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 523 5 1 4 6.1 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)NCc3cccc(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4295212 167372 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 523 5 1 4 6.1 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)NCc3cccc(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
71460577 81877 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 500 4 2 4 3.9 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)c(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164829 81877 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 500 4 2 4 3.9 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)c(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
16113902 137651 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL375859 137651 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
71462274 81820 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 528 5 2 4 3.8 CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1=O 10.1016/j.bmc.2012.07.018
CHEMBL2164506 81820 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 528 5 2 4 3.8 CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1=O 10.1016/j.bmc.2012.07.018
CHEMBL509976 215557 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human ghrelin receptor Ser3:08Ala(Ser123) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Ser3:08Ala(Ser123) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
70683143 73167 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 574 8 2 5 5.3 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(Cl)cc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011821 73167 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 574 8 2 5 5.3 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(Cl)cc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
46880495 6337 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)C[C@@H]3C)cc2)c1 10.1016/j.bmcl.2010.01.043
CHEMBL1082162 6337 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)C[C@@H]3C)cc2)c1 10.1016/j.bmcl.2010.01.043
11697618 62569 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 427 6 1 4 5.5 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Br)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178289 62569 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 427 6 1 4 5.5 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Br)noc2C)cc1 10.1016/j.bmcl.2004.11.075
145988557 167236 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 523 4 1 2 6.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C#CC3CC3)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4292914 167236 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 523 4 1 2 6.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C#CC3CC3)c(Cl)c2Cl)CC1 10.1021/acs.jmedchem.8b00794
44409771 141228 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 461 6 3 7 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@@H]3CC4C=CC3C4)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL383073 141228 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 461 6 3 7 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@@H]3CC4C=CC3C4)cc2)cc1 10.1016/j.bmcl.2006.01.012
145980333 166557 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 577 6 1 4 7.5 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4280040 166557 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 577 6 1 4 7.5 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
11329138 64430 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at GHSR expressed in CHOK cells assessed as inhibition of ghrelin-induced increase in intracellular calcium levelAntagonist activity at GHSR expressed in CHOK cells assessed as inhibition of ghrelin-induced increase in intracellular calcium level
ChEMBL 481 9 1 5 5.1 CCN(CC)c1ccc(NC(=O)C2(N(C)C(=O)OCC(C)C)CCc3cccc(OC)c3C2)cc1 10.1021/jm0491750
CHEMBL181350 64430 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at GHSR expressed in CHOK cells assessed as inhibition of ghrelin-induced increase in intracellular calcium levelAntagonist activity at GHSR expressed in CHOK cells assessed as inhibition of ghrelin-induced increase in intracellular calcium level
ChEMBL 481 9 1 5 5.1 CCN(CC)c1ccc(NC(=O)C2(N(C)C(=O)OCC(C)C)CCc3cccc(OC)c3C2)cc1 10.1021/jm0491750
44576247 214199 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inverse agonist activity at human ghrelin receptor Met5:05Ala(Met213) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Met5:05Ala(Met213) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 214199 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inverse agonist activity at human ghrelin receptor Met5:05Ala(Met213) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Met5:05Ala(Met213) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
11568561 169530 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 447 7 1 5 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(OC)c1 10.1016/j.bmcl.2004.11.075
CHEMBL443560 169530 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 447 7 1 5 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(OC)c1 10.1016/j.bmcl.2004.11.075
145991945 166791 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 615 6 1 4 7.8 CCN(C(=O)N[C@@H](C)c1ccc(C#CC2CC2)c(Cl)c1Cl)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1 10.1021/acs.jmedchem.8b00794
CHEMBL4284715 166791 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 615 6 1 4 7.8 CCN(C(=O)N[C@@H](C)c1ccc(C#CC2CC2)c(Cl)c1Cl)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1 10.1021/acs.jmedchem.8b00794
44394982 66108 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cellsAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells
ChEMBL 523 9 1 6 5.7 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL184093 66108 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cellsAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells
ChEMBL 523 9 1 6 5.7 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)CC1 10.1016/j.bmcl.2004.06.060
66788278 125166 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645254 125166 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
56942099 125168 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645256 125168 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
56942243 125170 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645258 125170 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 10.1016/j.bmcl.2016.04.003
127045858 139837 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 618 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2=CCCCO2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799225 139837 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 618 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2=CCCCO2)cc1 10.1016/j.bmcl.2016.04.003
70681018 73165 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 554 8 2 5 5.0 Cc1ccccc1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
CHEMBL2011819 73165 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 554 8 2 5 5.0 Cc1ccccc1Oc1ccc2c(c1)C(=O)N([C@@H](C(=O)NC1CCN(Cc3ccccc3)CC1)C(C)C)CC(=O)N2 10.1016/j.bmcl.2012.01.014
70685225 73199 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 576 8 2 5 5.0 CC(C)[C@H](C(=O)N1CCC(NCc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011894 73199 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 576 8 2 5 5.0 CC(C)[C@H](C(=O)N1CCC(NCc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
11410373 138510 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 558 10 4 8 4.2 Cc1cc(C)cc(CNC(=O)CCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)c1 10.1016/j.bmcl.2006.01.012
CHEMBL377514 138510 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 558 10 4 8 4.2 Cc1cc(C)cc(CNC(=O)CCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)c1 10.1016/j.bmcl.2006.01.012
11339816 75978 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 446 8 3 7 4.7 Nc1nc(N)c(-c2ccc(NCc3ccnc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205521 75978 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 446 8 3 7 4.7 Nc1nc(N)c(-c2ccc(NCc3ccnc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
145992253 166904 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 595 6 1 6 6.4 COC(=O)c1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4286849 166904 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 595 6 1 6 6.4 COC(=O)c1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(-c5cc(C)ncn5)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
11503585 65174 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 461 9 2 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCCO)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL182542 65174 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 461 9 2 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCCO)cc1 10.1016/j.bmcl.2004.06.060
44409762 75857 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 441 9 4 8 2.7 CCc1nc(N)nc(NCCO)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204884 75857 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 441 9 4 8 2.7 CCc1nc(N)nc(NCCO)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122180026 121561 0 None 8 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against ghrelin receptor (unknown origin) expressed in CHO cells assessed as inhibition of ghrelin-induced calcium responseAntagonist activity against ghrelin receptor (unknown origin) expressed in CHO cells assessed as inhibition of ghrelin-induced calcium response
ChEMBL 566 7 2 7 4.4 CC(=O)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586032 121561 0 None 8 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against ghrelin receptor (unknown origin) expressed in CHO cells assessed as inhibition of ghrelin-induced calcium responseAntagonist activity against ghrelin receptor (unknown origin) expressed in CHO cells assessed as inhibition of ghrelin-induced calcium response
ChEMBL 566 7 2 7 4.4 CC(=O)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
46880846 7580 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 442 3 1 3 4.4 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1088038 7580 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 442 3 1 3 4.4 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
44389248 122142 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 433 7 2 5 5.0 CCN(CCO)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL359714 122142 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 433 7 2 5 5.0 CCN(CCO)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
70695749 73181 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 562 9 2 6 4.3 CC(C)[C@H](C(=O)N1CCC(NCCC2CCOCC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011836 73181 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 562 9 2 6 4.3 CC(C)[C@H](C(=O)N1CCC(NCCC2CCOCC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
122178614 121325 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 660 13 2 7 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2C(=O)c2ccccc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581047 121325 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 660 13 2 7 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2C(=O)c2ccccc2)cc1 10.1016/j.bmcl.2014.11.031
70695748 73173 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 498 7 2 5 3.7 O=C1CN(CC(=O)NC2CCN(Cc3ccccc3)CC2)C(=O)c2cc(Oc3ccccc3)ccc2N1 10.1016/j.bmcl.2012.01.014
CHEMBL2011827 73173 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 498 7 2 5 3.7 O=C1CN(CC(=O)NC2CCN(Cc3ccccc3)CC2)C(=O)c2cc(Oc3ccccc3)ccc2N1 10.1016/j.bmcl.2012.01.014
145981687 166553 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 509 5 1 3 6.5 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(Cl)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4279987 166553 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 509 5 1 3 6.5 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(Cl)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
11508639 76506 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(Cl)cc2)cc1 10.1021/jm0510934
CHEMBL206091 76506 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(Cl)cc2)cc1 10.1021/jm0510934
44409683 76230 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 480 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205848 76230 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 480 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11626181 124355 2 None - 1 Human 6.5 pIC50 = 6.5 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 431 7 1 4 6.3 CCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL363896 124355 2 None - 1 Human 6.5 pIC50 = 6.5 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 431 7 1 4 6.3 CCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
11690097 76643 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 411 6 2 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(N(C)Cc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
CHEMBL206446 76643 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 411 6 2 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(N(C)Cc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
44409775 75996 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 8 3 7 3.7 CCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205605 75996 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 8 3 7 3.7 CCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44576247 214199 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inverse agonist activity at human wild type ghrelin receptor expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human wild type ghrelin receptor expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 214199 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inverse agonist activity at human wild type ghrelin receptor expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human wild type ghrelin receptor expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
11655355 74392 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)s3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL202642 74392 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)s3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
127047654 139952 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799883 139952 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
16113799 168689 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL436849 168689 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
145986080 166428 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 489 5 1 3 6.2 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(C)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4277793 166428 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 489 5 1 3 6.2 COc1ccc([C@H](C)NC(=O)N(C)C2CCN(C3CCc4cc(C)ccc43)CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
56942385 125172 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645260 125172 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
46880771 5878 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 448 3 1 4 4.4 C[C@H]1CN(C(=O)c2csc(-c3ccccc3F)n2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1079623 5878 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 448 3 1 4 4.4 C[C@H]1CN(C(=O)c2csc(-c3ccccc3F)n2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
11654867 76172 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 429 7 3 5 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(CCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205833 76172 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 429 7 3 5 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(CCc2ccccc2)n1 10.1021/jm0510934
122178600 121310 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581033 121310 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2)cc1 10.1016/j.bmcl.2014.11.031
46880844 7564 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 432 3 1 4 3.0 C[C@H]1CN(C(=O)c2ccc(N3CCOCC3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1087907 7564 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 432 3 1 4 3.0 C[C@H]1CN(C(=O)c2ccc(N3CCOCC3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
11248021 139230 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 454 8 4 6 4.3 Nc1nc(N)c(-c2ccc(NC(=O)NCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL378989 139230 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 454 8 4 6 4.3 Nc1nc(N)c(-c2ccc(NC(=O)NCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
122182189 121982 0 None -7 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assayAntagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assay
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593814 121982 0 None -7 2 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assayAntagonist activity at rat ghrelin receptor expressed in CHO cells assessed as blocking of human ghrelin-induced response by FLIPR based intracellular Ca2+ mobilization assay
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
44409865 140693 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 500 7 3 8 3.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN3Cc4ccccc4C3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL381759 140693 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 500 7 3 8 3.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN3Cc4ccccc4C3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11751384 141481 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 453 9 3 6 4.6 Nc1nc(N)c(-c2ccc(NC(=O)CCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL384524 141481 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 453 9 3 6 4.6 Nc1nc(N)c(-c2ccc(NC(=O)CCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
44409679 75479 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 466 8 4 8 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204322 75479 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 466 8 4 8 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409868 76713 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 487 9 3 7 4.9 CCc1nc(N)nc(NCc2ccccc2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206673 76713 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 487 9 3 7 4.9 CCc1nc(N)nc(NCc2ccccc2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409667 75940 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 451 6 3 7 4.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CCCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205294 75940 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 451 6 3 7 4.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3CCCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44576247 214199 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 214199 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
56942388 139918 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799687 139918 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
11166495 75521 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 437 8 2 7 4.5 N#Cc1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL204474 75521 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 437 8 2 7 4.5 N#Cc1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
145994050 167321 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 615 6 1 6 7.1 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4294493 167321 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 615 6 1 6 7.1 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
11538533 74972 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203280 74972 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
46880770 5877 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 458 3 1 3 4.9 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3Cl)cn2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1079622 5877 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 458 3 1 3 4.9 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3Cl)cn2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
71453390 81814 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 526 6 2 4 4.4 C=CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164500 81814 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 526 6 2 4 4.4 C=CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
44409763 141340 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 487 6 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3Cc4ccccc4O3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL383757 141340 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 487 6 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3C3Cc4ccccc4O3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409989 165802 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 467 11 3 7 4.8 CCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL424860 165802 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 467 11 3 7 4.8 CCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44410008 141226 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 9 2 7 4.2 CCc1nc(N)nc(N(CC)CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL383058 141226 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 9 2 7 4.2 CCc1nc(N)nc(N(CC)CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11178309 79872 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 445 8 3 7 4.3 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL212415 79872 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 445 8 3 7 4.3 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
11517629 168314 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 431 6 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C)c1 10.1016/j.bmcl.2004.11.075
CHEMBL434330 168314 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 431 6 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C)c1 10.1016/j.bmcl.2004.11.075
127047655 139589 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797531 139589 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
127046957 139682 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 649 12 3 7 5.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc(F)cc(F)n2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798155 139682 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 649 12 3 7 5.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc(F)cc(F)n2)cc1 10.1016/j.bmcl.2016.04.003
127045858 139837 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 618 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2=CCCCO2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799225 139837 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 618 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2=CCCCO2)cc1 10.1016/j.bmcl.2016.04.003
56942098 125167 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645255 125167 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
127046957 139682 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 649 12 3 7 5.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc(F)cc(F)n2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798155 139682 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 649 12 3 7 5.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc(F)cc(F)n2)cc1 10.1016/j.bmcl.2016.04.003
46880630 6066 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 491 3 1 2 5.8 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3C(F)(F)F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080735 6066 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 491 3 1 2 5.8 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3C(F)(F)F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
70685219 73180 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 560 9 2 5 5.4 CC(C)[C@H](C(=O)N1CCC(NCCC2CCCCC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011835 73180 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 560 9 2 5 5.4 CC(C)[C@H](C(=O)N1CCC(NCCC2CCCCC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
16113245 121308 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581030 121308 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2014.11.031
122178607 121318 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 592 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncc(F)cc2F)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581040 121318 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 592 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncc(F)cc2F)cc1 10.1016/j.bmcl.2014.11.031
11452801 139273 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 417 7 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)C3CCCC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL379191 139273 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 417 7 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)C3CCCC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
46882763 5596 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-stimulated intracellular calcium mobilizationAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-stimulated intracellular calcium mobilization
ChEMBL 612 17 6 7 5.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1077617 5596 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-stimulated intracellular calcium mobilizationAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-stimulated intracellular calcium mobilization
ChEMBL 612 17 6 7 5.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
44409776 77114 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 7 3 7 3.5 CC(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL207754 77114 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 7 3 7 3.5 CC(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145991797 166892 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 613 5 1 6 6.5 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)NCc4ccc(-c5cnccn5)c(Cl)c4Cl)CC3)C2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4286597 166892 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 613 5 1 6 6.5 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)NCc4ccc(-c5cnccn5)c(Cl)c4Cl)CC3)C2)ncn1 10.1021/acs.jmedchem.8b00794
122178616 121326 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc3ccccc3cn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581048 121326 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc3ccccc3cn2)cc1 10.1016/j.bmcl.2014.11.031
11430583 80188 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 439 8 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL213704 80188 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 439 8 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL509976 215557 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human ghrelin receptor Phe3:04Ser(phe119) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Phe3:04Ser(phe119) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
11669486 64584 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 445 7 1 4 6.6 CCc1cc(N(CC)CC)ccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
CHEMBL181736 64584 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 445 7 1 4 6.6 CCc1cc(N(CC)CC)ccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
44409946 139790 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 514 7 3 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN3CCc4ccccc4C3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL379887 139790 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 514 7 3 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN3CCc4ccccc4C3)cc2)cc1 10.1016/j.bmcl.2006.01.012
127046806 139908 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 638 13 4 7 5.4 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799604 139908 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 638 13 4 7 5.4 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
122178600 121310 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581033 121310 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2)cc1 10.1016/j.bmcl.2014.11.031
11605333 76696 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 475 6 3 7 3.6 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Br)c1 10.1021/jm0510934
CHEMBL206589 76696 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 475 6 3 7 3.6 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Br)c1 10.1021/jm0510934
46880845 7579 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 460 3 1 3 4.5 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3F)c(F)c2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1088037 7579 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 460 3 1 3 4.5 C[C@H]1CN(C(=O)c2ccc(-c3ccncc3F)c(F)c2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
46880773 6175 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3ccccn3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1081301 6175 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 424 3 1 3 4.2 C[C@H]1CN(C(=O)c2ccc(-c3ccccn3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
122178604 121314 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2N)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581037 121314 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2N)cc1 10.1016/j.bmcl.2014.11.031
56942387 139637 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 579 13 4 7 4.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797857 139637 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 579 13 4 7 4.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
44576247 214199 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inverse agonist activity at human ghrelin receptor Ile4:20Ala(Ile178) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ile4:20Ala(Ile178) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 214199 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inverse agonist activity at human ghrelin receptor Ile4:20Ala(Ile178) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ile4:20Ala(Ile178) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
11683469 76677 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 433 6 3 7 3.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(C)(=O)=O)c(F)c2)cc1 10.1021/jm0510934
CHEMBL206486 76677 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 433 6 3 7 3.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(C)(=O)=O)c(F)c2)cc1 10.1021/jm0510934
44389216 123828 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 442 6 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C#N)c1 10.1016/j.bmcl.2004.11.075
CHEMBL362595 123828 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 442 6 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C#N)c1 10.1016/j.bmcl.2004.11.075
145979819 166449 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 655 8 1 6 7.9 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4278185 166449 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 655 8 1 6 7.9 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
46880498 5963 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 507 4 1 3 5.7 C[C@H]1CN(C(=O)c2ccc(-c3cccc(OC(F)(F)F)c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080155 5963 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 507 4 1 3 5.7 C[C@H]1CN(C(=O)c2ccc(-c3cccc(OC(F)(F)F)c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
71462273 81819 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 513 5 2 3 5.7 CCN1CCCC(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)C1 10.1016/j.bmc.2012.07.018
CHEMBL2164505 81819 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 513 5 2 3 5.7 CCN1CCCC(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)C1 10.1016/j.bmc.2012.07.018
71453404 81874 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)N[C@]2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164826 81874 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)N[C@]2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
44389283 62915 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 403 5 1 4 5.7 CCN(C)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178494 62915 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 403 5 1 4 5.7 CCN(C)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
11179347 77324 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 490 9 2 8 4.0 CS(=O)(=O)c1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL208477 77324 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 490 9 2 8 4.0 CS(=O)(=O)c1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
44409764 77120 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 488 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL207792 77120 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 488 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11606121 64546 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 523 6 2 6 5.9 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.11.075
CHEMBL181584 64546 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 523 6 2 6 5.9 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.11.075
11539587 67047 1 None - 1 Human 6.3 pIC50 = 6.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 445 8 1 4 6.7 CCCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL187271 67047 1 None - 1 Human 6.3 pIC50 = 6.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 445 8 1 4 6.7 CCCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL3586019 211778 6 None - 1 Rat 8.3 pIC50 = 8.3 Functional
Inverse agonist activity at rat ghrelin receptor by inositol phosphate turnover assayInverse agonist activity at rat ghrelin receptor by inositol phosphate turnover assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CCCNC(=N)N)C(N)=O 10.1016/j.bmcl.2015.04.040
122178608 121319 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 570 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(C)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581041 121319 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 570 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(C)n2)cc1 10.1016/j.bmcl.2014.11.031
44409821 76008 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 564 10 4 8 4.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CCC(=O)NCc3cccc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205711 76008 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 564 10 4 8 4.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CCC(=O)NCc3cccc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11340044 141310 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(NCc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL383522 141310 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(NCc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
70683149 73194 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 504 8 2 5 3.9 CC(C)[C@H](C(=O)N1CCC(NCC2CC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011887 73194 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 504 8 2 5 3.9 CC(C)[C@H](C(=O)N1CCC(NCC2CC2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
71452183 83500 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at ghrelin receptor assessed as inhibition of ghrelin-induced Ca2+ release by cell based assayAntagonist activity at ghrelin receptor assessed as inhibition of ghrelin-induced Ca2+ release by cell based assay
ChEMBL 538 5 4 6 1.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)N(C)C1=O 10.1021/jm1012374
CHEMBL2203623 83500 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at ghrelin receptor assessed as inhibition of ghrelin-induced Ca2+ release by cell based assayAntagonist activity at ghrelin receptor assessed as inhibition of ghrelin-induced Ca2+ release by cell based assay
ChEMBL 538 5 4 6 1.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)N(C)C1=O 10.1021/jm1012374
122178602 121312 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2Br)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581035 121312 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2Br)cc1 10.1016/j.bmcl.2014.11.031
11582836 62883 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 431 7 1 4 6.4 CCCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178463 62883 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 431 7 1 4 6.4 CCCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44389192 168622 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 471 4 1 4 6.2 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCCC1 10.1016/j.bmcl.2004.11.075
CHEMBL436275 168622 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 471 4 1 4 6.2 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCCC1 10.1016/j.bmcl.2004.11.075
71455106 81884 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 442 5 2 5 2.2 COc1ccc(C2(NC(=O)CN3CCN(C)CC3)C(=O)Nc3cc(Cl)c(C)cc32)cc1 10.1016/j.bmc.2012.07.018
CHEMBL2164835 81884 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 442 5 2 5 2.2 COc1ccc(C2(NC(=O)CN3CCN(C)CC3)C(=O)Nc3cc(Cl)c(C)cc32)cc1 10.1016/j.bmc.2012.07.018
44409998 138511 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 413 7 3 8 2.5 COCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL377515 138511 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 413 7 3 8 2.5 COCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145984632 166367 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 629 5 1 4 8.0 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)C(C)(C)C2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4276775 166367 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 629 5 1 4 8.0 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)C(C)(C)C2)ncn1 10.1021/acs.jmedchem.8b00794
10415364 126741 0 None -5 3 Human 7.3 pIC50 = 7.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL365294 126741 0 None -5 3 Human 7.3 pIC50 = 7.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
15949382 74819 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 6 3 8 3.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@@H]3CCCO3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203158 74819 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 6 3 8 3.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@@H]3CCCO3)cc2)cc1 10.1016/j.bmcl.2006.01.012
145993313 166868 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 577 7 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3cccc(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4286101 166868 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 577 7 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](CC3CC3)c3cccc(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
11605822 124362 1 None - 1 Human 7.3 pIC50 = 7.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 503 9 1 6 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL363930 124362 1 None - 1 Human 7.3 pIC50 = 7.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 503 9 1 6 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCO2)cc1 10.1016/j.bmcl.2004.06.060
11154001 79859 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 406 7 4 6 3.6 CC(C)NC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
CHEMBL212354 79859 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 406 7 4 6 3.6 CC(C)NC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
44394930 66302 1 None - 1 Human 6.3 pIC50 = 6.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2cccc3c2OCO3)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL185028 66302 1 None - 1 Human 6.3 pIC50 = 6.3 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2cccc3c2OCO3)cc1 10.1016/j.bmcl.2004.06.060
11699004 66173 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 501 9 1 5 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL184429 66173 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 501 9 1 5 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)cc1 10.1016/j.bmcl.2004.06.060
11618705 166914 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 423 6 1 4 5.3 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL428698 166914 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 423 6 1 4 5.3 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)CC1 10.1016/j.bmcl.2004.06.060
44409785 75774 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 6 3 8 3.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@H]3CCCO3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204852 75774 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 439 6 3 8 3.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@H]3CCCO3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409990 76488 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 481 12 3 7 5.2 CCCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205995 76488 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 481 12 3 7 5.2 CCCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145992125 166726 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 552 5 2 5 6.2 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(N)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4283504 166726 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 552 5 2 5 6.2 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(N)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
46880568 6356 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 423 3 1 2 4.8 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1082211 6356 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 423 3 1 2 4.8 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
70687383 73195 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 525 9 2 4 6.6 CC(C)[C@H](C[C@H]1CC[C@@H](NCc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011890 73195 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 525 9 2 4 6.6 CC(C)[C@H](C[C@H]1CC[C@@H](NCc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
16113245 121308 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581030 121308 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL509976 215557 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Agonist activity at human ghrelin receptor Ser4:16Ala(Ser174) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Ser4:16Ala(Ser174) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
57422817 113422 18 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL 620 8 2 10 3.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/acs.jmedchem.1c02191
CHEMBL3319223 113422 18 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inverse agonist activity at GHS-R1a (unknown origin)Inverse agonist activity at GHS-R1a (unknown origin)
ChEMBL 620 8 2 10 3.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/acs.jmedchem.1c02191
11190594 75956 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 469 10 3 8 3.9 CC(C)CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205445 75956 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 469 10 3 8 3.9 CC(C)CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
56942385 125172 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645260 125172 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
44576247 214199 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inverse agonist activity at human ghrelin receptor Phe3:04Ser(phe119) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Phe3:04Ser(phe119) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 214199 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inverse agonist activity at human ghrelin receptor Phe3:04Ser(phe119) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Phe3:04Ser(phe119) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
16113904 137011 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 550 12 3 6 5.1 COc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL374655 137011 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 550 12 3 6 5.1 COc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
44389215 63048 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccc(Cl)cc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178838 63048 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccc(Cl)cc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44576247 214199 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inverse agonist activity at human ghrelin receptor Asn7:02Ala(Asn305) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Asn7:02Ala(Asn305) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 214199 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inverse agonist activity at human ghrelin receptor Asn7:02Ala(Asn305) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Asn7:02Ala(Asn305) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
44409809 75036 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 10 3 7 4.4 CCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203578 75036 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 10 3 7 4.4 CCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
16113468 141775 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL386218 141775 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
11531313 62474 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 394 7 1 6 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3[N+](=O)[O-])noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178137 62474 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 394 7 1 6 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3[N+](=O)[O-])noc2C)cc1 10.1016/j.bmcl.2004.11.075
44389167 123832 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 425 7 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL362612 123832 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 425 7 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
46880674 6110 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccc(F)cc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080926 6110 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccc(F)cc3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
71455085 81815 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 4 2 4 4.3 CN1CCCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164501 81815 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 4 2 4 4.3 CN1CCCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
46880463 6236 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)[C@H](C)C3)cc2)c1 10.1016/j.bmcl.2010.01.043
CHEMBL1081649 6236 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)[C@H](C)C3)cc2)c1 10.1016/j.bmcl.2010.01.043
46880812 5989 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 430 3 1 4 4.3 C[C@H]1CN(C(=O)c2ccc(-c3cncs3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080320 5989 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 430 3 1 4 4.3 C[C@H]1CN(C(=O)c2ccc(-c3cncs3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
46880497 6339 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 423 3 1 2 4.8 O=C(c1ccc(-c2ccccc2)cc1)N1CCCN(C(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/j.bmcl.2010.01.043
CHEMBL1082164 6339 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 423 3 1 2 4.8 O=C(c1ccc(-c2ccccc2)cc1)N1CCCN(C(=O)c2ccc3cc[nH]c3c2)CC1 10.1016/j.bmcl.2010.01.043
44409770 141343 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 461 6 3 7 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@H]3CC4C=CC3C4)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL383766 141343 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 461 6 3 7 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3[C@H]3CC4C=CC3C4)cc2)cc1 10.1016/j.bmcl.2006.01.012
122178604 121314 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2N)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581037 121314 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2N)cc1 10.1016/j.bmcl.2014.11.031
46880496 6338 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)C[C@H]3C)cc2)c1 10.1016/j.bmcl.2010.01.043
CHEMBL1082163 6338 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1cccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)C[C@H]3C)cc2)c1 10.1016/j.bmcl.2010.01.043
CHEMBL502208 214127 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1074/jbc.m609796200
145980382 166619 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4281310 166619 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
44389186 64585 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 379 7 1 5 4.8 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3OC)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL181739 64585 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 379 7 1 5 4.8 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3OC)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44409864 75470 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 502 9 3 8 4.0 CN(Cc1ccccc1)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204266 75470 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 502 9 3 8 4.0 CN(Cc1ccccc1)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409975 75761 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 411 7 3 7 3.3 CCc1nc(N)nc(NC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204835 75761 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 411 7 3 7 3.3 CCc1nc(N)nc(NC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409455 75939 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 487 6 3 7 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c2)cc1 10.1021/jm0510934
CHEMBL205286 75939 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 487 6 3 7 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c2)cc1 10.1021/jm0510934
11441554 220 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 420 6 4 6 3.9 O=C(NC(C)(C)C)Nc1ccc(cc1)c1c(N)nc(nc1COCc1ccccc1)N 10.1021/jm060461g
5871 220 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 420 6 4 6 3.9 O=C(NC(C)(C)C)Nc1ccc(cc1)c1c(N)nc(nc1COCc1ccccc1)N 10.1021/jm060461g
CHEMBL212761 220 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 420 6 4 6 3.9 O=C(NC(C)(C)C)Nc1ccc(cc1)c1c(N)nc(nc1COCc1ccccc1)N 10.1021/jm060461g
11340329 79573 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 468 9 4 6 4.4 Nc1nc(N)c(-c2ccc(NC(=O)NCCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL211454 79573 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 468 9 4 6 4.4 Nc1nc(N)c(-c2ccc(NC(=O)NCCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
122178605 121315 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581038 121315 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2014.11.031
127047655 139589 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797531 139589 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
46880672 6164 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1ccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)[C@@H](C)C3)cc2)cc1 10.1016/j.bmcl.2010.01.043
CHEMBL1081254 6164 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 453 4 1 3 4.8 COc1ccc(-c2ccc(C(=O)N3CCN(C(=O)c4ccc5cc[nH]c5c4)[C@@H](C)C3)cc2)cc1 10.1016/j.bmcl.2010.01.043
66601728 81812 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 5 2 4 4.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164499 81812 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 514 5 2 4 4.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
70689440 73164 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 554 8 2 5 5.0 Cc1ccc(Oc2ccc3c(c2)C(=O)N([C@@H](C(=O)NC2CCN(Cc4ccccc4)CC2)C(C)C)CC(=O)N3)cc1 10.1016/j.bmcl.2012.01.014
CHEMBL2011818 73164 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 554 8 2 5 5.0 Cc1ccc(Oc2ccc3c(c2)C(=O)N([C@@H](C(=O)NC2CCN(Cc4ccccc4)CC2)C(C)C)CC(=O)N3)cc1 10.1016/j.bmcl.2012.01.014
70693644 73198 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 496 9 1 3 6.7 CC(C)[C@H](C[C@H]1CC[C@@H](NCC2CC2)CC1)N1CCc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011893 73198 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 496 9 1 3 6.7 CC(C)[C@H](C[C@H]1CC[C@@H](NCC2CC2)CC1)N1CCc2ccc(Oc3ccc(F)cc3F)cc2C1=O 10.1016/j.bmcl.2012.01.014
70695747 73162 0 None 1 2 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse GHSR1 receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at mouse GHSR1 receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011816 73162 0 None 1 2 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse GHSR1 receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at mouse GHSR1 receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
11225576 166013 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL425594 166013 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11225576 166013 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL425594 166013 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
122178608 121319 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 570 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(C)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581041 121319 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 570 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(C)n2)cc1 10.1016/j.bmcl.2014.11.031
122178609 121320 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 586 12 2 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(OC)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581042 121320 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 586 12 2 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(OC)n2)cc1 10.1016/j.bmcl.2014.11.031
56942388 139918 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799687 139918 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
56942535 139736 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 593 12 4 7 4.4 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798525 139736 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 593 12 4 7 4.4 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
11176805 77305 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 391 7 3 6 4.5 CC(C)(C)CNc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm0510934
CHEMBL208374 77305 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 391 7 3 6 4.5 CC(C)(C)CNc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm0510934
71453405 81882 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 462 5 2 5 2.6 COc1ccc(C2(NC(=O)CN3CCN(C)CC3)C(=O)Nc3cc(Cl)c(Cl)cc32)cc1 10.1016/j.bmc.2012.07.018
CHEMBL2164833 81882 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 462 5 2 5 2.6 COc1ccc(C2(NC(=O)CN3CCN(C)CC3)C(=O)Nc3cc(Cl)c(Cl)cc32)cc1 10.1016/j.bmc.2012.07.018
44394913 127147 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 537 10 1 5 7.5 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccccc2OC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL365721 127147 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 537 10 1 5 7.5 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccccc2OC)cc1 10.1016/j.bmcl.2004.06.060
44409832 76381 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 398 6 4 8 1.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205955 76381 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 398 6 4 8 1.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN)cc2)cc1 10.1016/j.bmcl.2006.01.012
25190383 81880 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164831 81880 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assayAntagonist activity at human GHSR1 expressed in CHO-CREluc cells after 4 hrs by Luciferase reporter assay
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
122178615 121278 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2nccc3ccccc23)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3580668 121278 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2nccc3ccccc23)cc1 10.1016/j.bmcl.2014.11.031
44410013 77024 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 10 3 7 4.5 CCCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL207268 77024 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 453 10 3 7 4.5 CCCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44389243 64553 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 557 7 1 6 6.2 O=C(Nc1ccccc1C(=O)N1CCCCC1)c1c(-c2c(Cl)cccc2Cl)noc1CCC1OCCCO1 10.1016/j.bmcl.2004.11.075
CHEMBL181619 64553 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 557 7 1 6 6.2 O=C(Nc1ccccc1C(=O)N1CCCCC1)c1c(-c2c(Cl)cccc2Cl)noc1CCC1OCCCO1 10.1016/j.bmcl.2004.11.075
753168 123213 40 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 349 6 1 4 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL361366 123213 40 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assayInhibition of ghrelin-induced increase of intracellular [Ca2+] in CHO K cell FLIPR assay
ChEMBL 349 6 1 4 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
46880566 6354 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 491 3 1 2 5.8 C[C@H]1CN(C(=O)c2ccc(-c3cccc(C(F)(F)F)c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1082209 6354 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 491 3 1 2 5.8 C[C@H]1CN(C(=O)c2ccc(-c3cccc(C(F)(F)F)c3)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
122178603 121313 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 590 11 2 6 6.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(Cl)nc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581036 121313 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 590 11 2 6 6.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(Cl)nc2)cc1 10.1016/j.bmcl.2014.11.031
44409979 140534 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 7 2 7 3.4 CCc1nc(N)nc(N(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL381159 140534 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 425 7 2 7 3.4 CCc1nc(N)nc(N(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11256439 75350 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 344 5 3 6 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C#N)cc2)cc1 10.1021/jm0510934
CHEMBL203843 75350 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 344 5 3 6 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C#N)cc2)cc1 10.1021/jm0510934
11655578 170009 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 462 8 3 7 5.2 Nc1nc(N)c(-c2ccc(NCc3cnc4ccccc4c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL444277 170009 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 462 8 3 7 5.2 Nc1nc(N)c(-c2ccc(NCc3cnc4ccccc4c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
70681019 73170 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 570 9 2 6 4.7 COc1ccc(Oc2ccc3c(c2)C(=O)N([C@@H](C(=O)NC2CCN(Cc4ccccc4)CC2)C(C)C)CC(=O)N3)cc1 10.1016/j.bmcl.2012.01.014
CHEMBL2011824 73170 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 570 9 2 6 4.7 COc1ccc(Oc2ccc3c(c2)C(=O)N([C@@H](C(=O)NC2CCN(Cc4ccccc4)CC2)C(C)C)CC(=O)N3)cc1 10.1016/j.bmcl.2012.01.014
122178612 121323 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 572 11 2 6 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc[n+]2[O-])cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581045 121323 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 572 11 2 6 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc[n+]2[O-])cc1 10.1016/j.bmcl.2014.11.031
11617435 75968 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 359 5 3 6 4.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2csc(Cl)c2)cc1 10.1021/jm0510934
CHEMBL205486 75968 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 359 5 3 6 4.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2csc(Cl)c2)cc1 10.1021/jm0510934
145988647 167048 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4ncccn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4289530 167048 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4ncccn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
11663710 124441 1 None - 1 Human 8.1 pIC50 = 8.1 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 528 9 1 5 6.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL363995 124441 1 None - 1 Human 8.1 pIC50 = 8.1 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 528 9 1 5 6.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
56942099 125168 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645256 125168 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
56942242 125169 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645257 125169 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 10.1016/j.bmcl.2016.04.003
11663710 124441 1 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilizationAntagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilization
ChEMBL 528 9 1 5 6.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)cc1 10.1016/j.bmcl.2012.01.014
CHEMBL363995 124441 1 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilizationAntagonist activity at human GHSR1a receptor assessed as blockade of intracellular Ca2+ mobilization
ChEMBL 528 9 1 5 6.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)cc1 10.1016/j.bmcl.2012.01.014
70695747 73162 0 None -1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011816 73162 0 None -1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
70687380 73176 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)N1CCC(NCc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011831 73176 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assayAntagonist activity at human GHSR1a receptor assessed as intracellular Ca2+ concentration by aequorin luminescent assay
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)N1CCC(NCc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
122178605 121315 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581038 121315 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2014.11.031
145988894 167120 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4290680 167120 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1 10.1021/acs.jmedchem.8b00794
16203569 141708 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL385803 141708 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
145981343 166685 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 669 6 1 6 7.6 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@H](c3ccc(-c4cnccn4)c(Cl)c3Cl)C(F)(F)F)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL4282719 166685 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 669 6 1 6 7.6 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@H](c3ccc(-c4cnccn4)c(Cl)c3Cl)C(F)(F)F)CC2)ncn1 10.1021/acs.jmedchem.8b00794
CHEMBL509976 215557 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human ghrelin receptor Phe7:06Leu(Phe306) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulationAgonist activity at human ghrelin receptor Phe7:06Leu(Phe306) mutant expressed in african green monkey COS7 cells assessed as stimulation of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
122178615 121278 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2nccc3ccccc23)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3580668 121278 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2nccc3ccccc23)cc1 10.1016/j.bmcl.2014.11.031
44409810 140875 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 469 9 3 9 2.8 CCOC(=O)CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL382138 140875 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 469 9 3 9 2.8 CCOC(=O)CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
16113124 121309 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccncc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581032 121309 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccncc2)cc1 10.1016/j.bmcl.2014.11.031
44576247 214199 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inverse agonist activity at human ghrelin receptor Ser5:09Ala(Ser217) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ser5:09Ala(Ser217) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 214199 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inverse agonist activity at human ghrelin receptor Ser5:09Ala(Ser217) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor Ser5:09Ala(Ser217) mutant expressed in african green monkey COS7 cells assessed as inhibition of constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
44409536 75480 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 579 9 3 8 5.2 Nc1nc(N)c(-c2ccc(NCc3cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL204325 75480 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 579 9 3 8 5.2 Nc1nc(N)c(-c2ccc(NCc3cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
145992835 166810 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cncnc4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4285075 166810 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 587 5 1 4 7.1 C[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cncnc4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
11327400 75343 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 412 8 3 7 4.0 Nc1nc(N)c(-c2ccc(NCc3ccncc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL203782 75343 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 412 8 3 7 4.0 Nc1nc(N)c(-c2ccc(NCc3ccncc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
11539588 66883 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 445 7 1 4 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C(C)C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL186540 66883 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 445 7 1 4 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C(C)C)cc1 10.1016/j.bmcl.2004.06.060
16113796 84652 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL222518 84652 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilizationAntagonist activity at human GHSR1a receptor expressed in CHO cells assessed as reduction of ghrelin-induced intracellular calcium mobilization
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
11442040 78522 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 440 7 4 6 4.7 Nc1nc(N)c(-c2ccc(NC(=O)Nc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL211211 78522 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Activity at GHS receptor by calcium flux assay in CHO-K cellsActivity at GHS receptor by calcium flux assay in CHO-K cells
ChEMBL 440 7 4 6 4.7 Nc1nc(N)c(-c2ccc(NC(=O)Nc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
122178601 121311 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cncc(Br)c2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581034 121311 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilizationAntagonist activity at GHSR1a (unknown origin) assessed as inhibition of ghrelin-induced intracellular calcium mobilization
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cncc(Br)c2)cc1 10.1016/j.bmcl.2014.11.031
56942243 125170 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645258 125170 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipramAntagonist activity at human GHS-R1a transfected in mouse LTK cells after 6 hrs by CRE/luciferase reporter gene assay in presence of ghrelin and rolipram
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 10.1016/j.bmcl.2016.04.003
46880725 6227 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 455 3 1 2 5.3 Cc1ccccc1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1F 10.1016/j.bmcl.2010.01.043
CHEMBL1081612 6227 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 455 3 1 2 5.3 Cc1ccccc1-c1ccc(C(=O)N2CCN(C(=O)c3ccc4cc[nH]c4c3)[C@@H](C)C2)cc1F 10.1016/j.bmcl.2010.01.043
122178609 121320 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 586 12 2 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(OC)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581042 121320 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assayAntagonist activity at human GSHR1a expressed in mouse LTK cells assessed as inhibition of ghrelin-induced reporter gene expression after 6 hrs by CRE/luciferase reporter gene assay
ChEMBL 586 12 2 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(OC)n2)cc1 10.1016/j.bmcl.2014.11.031
11454617 141294 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 488 8 3 8 4.0 CN(Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2006.01.012
CHEMBL383411 141294 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 488 8 3 8 4.0 CN(Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2006.01.012
46880628 6000 0 None -4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
CHEMBL1080389 6000 0 None -4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assayAntagonist activity at human GHSR expressed in CHOK1 cells assessed as inhibition of ghrelin-induced intracellular calcium flux by aequorin flash luminescence assay
ChEMBL 441 3 1 2 5.0 C[C@H]1CN(C(=O)c2ccc(-c3ccccc3F)cc2)CCN1C(=O)c1ccc2cc[nH]c2c1 10.1016/j.bmcl.2010.01.043
44409684 140860 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 474 8 4 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL382033 140860 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 474 8 4 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409672 140462 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 479 9 3 9 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccco3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL380971 140462 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 479 9 3 9 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccco3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409673 76721 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 493 9 3 9 3.9 Cc1ccc(COCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)o1 10.1016/j.bmcl.2006.01.012
CHEMBL206741 76721 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 493 9 3 9 3.9 Cc1ccc(COCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)o1 10.1016/j.bmcl.2006.01.012
11453509 76149 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 441 9 3 7 4.6 COc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL205784 76149 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 441 9 3 7 4.6 COc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
127047362 139694 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 590 11 5 7 4.7 COc1ccc(Cn2c([C@H](N)Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798204 139694 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 590 11 5 7 4.7 COc1ccc(Cn2c([C@H](N)Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
56942535 139736 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 593 12 4 7 4.4 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798525 139736 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric methodAntagonist activity at human GHS-R1a transfected in CHO cells assessed as inhibition of ghrelin-induced intracellular calcium mobilization measured over 60 secs by fluo-4AM dye-based fluorometric method
ChEMBL 593 12 4 7 4.4 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
145990956 166997 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 509 4 1 2 6.6 C[C@H](NC(=O)N(C)C1CCN(C2CCc3ccccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
CHEMBL4288441 166997 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assayAntagonist activity at recombinant human GHSR1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced intracellular calcium release incubated for 20 secs and measured after 2 mins by FLIPR assay
ChEMBL 509 4 1 2 6.6 C[C@H](NC(=O)N(C)C1CCN(C2CCc3ccccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl 10.1021/acs.jmedchem.8b00794
44394947 169199 1 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL440939 169199 1 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)cc1 10.1016/j.bmcl.2004.06.060
44410007 76398 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 438 8 4 8 2.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205963 76398 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of human GHS receptor by FLIPRInhibition of human GHS receptor by FLIPR
ChEMBL 438 8 4 8 2.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11583811 75958 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 479 8 3 6 5.7 Nc1nc(N)c(-c2ccc(NCc3ccc(C(F)(F)F)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205450 75958 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 479 8 3 6 5.7 Nc1nc(N)c(-c2ccc(NCc3ccc(C(F)(F)F)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
11576960 67085 1 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 500 8 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL187427 67085 1 None - 1 Human 7.0 pIC50 = 7.0 Functional
Ability to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assayAbility to inhibit ghrelin induced increase in intracellular [Ca2+] in CHO-K cells was determined by FLIPR assay
ChEMBL 500 8 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
11281346 75989 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 411 8 3 6 4.6 Nc1nc(N)c(-c2ccc(NCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205568 75989 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cellsAntagonist activity at human GHS receptor by inhibition of ghrelin-induced intracellular calcium flux in CHOK cells
ChEMBL 411 8 3 6 4.6 Nc1nc(N)c(-c2ccc(NCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL499371 214072 0 None - 1 Human 6.0 pIC50 = 6 Functional
Inverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulationInverse agonist activity at human ghrelin receptor expressed in african green monkey COS7 cells assessed as constitutively stimulated inositol phosphate accumulation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCC(N)=O)C(N)=O 10.1074/jbc.m609796200
155540883 172933 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assayCompetitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4517399 172933 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assayCompetitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
155540883 172933 0 None - 1 Human 8.0 pKd = 8.0 Functional
Competitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assayCompetitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4517399 172933 0 None - 1 Human 8.0 pKd = 8.0 Functional
Competitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assayCompetitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
155557019 174563 0 None - 1 Human 7.5 pKd = 7.5 Functional
Competitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assayCompetitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4556887 174563 0 None - 1 Human 7.5 pKd = 7.5 Functional
Competitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assayCompetitive antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM after 30 mins by HTRF assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
155557019 174563 0 None - 1 Human 7.1 pKd = 7.1 Functional
Competitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assayCompetitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4556887 174563 0 None - 1 Human 7.1 pKd = 7.1 Functional
Competitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assayCompetitive antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM after 15 mins by Fluo 4-AM dye-based fluorescence assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
57399248 69015 0 None - 1 Human 9.0 pKi = 9 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm1012374
CHEMBL1923617 69015 0 None - 1 Human 9.0 pKi = 9 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm1012374
71452183 83500 0 None - 1 Human 7.0 pKi = 7 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 538 5 4 6 1.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)N(C)C1=O 10.1021/jm1012374
CHEMBL2203623 83500 0 None - 1 Human 7.0 pKi = 7 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 538 5 4 6 1.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CO)N(C)C1=O 10.1021/jm1012374
44454117 155532 0 None - 1 Human 7.9 pKi = 7.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
CHEMBL404336 155532 0 None - 1 Human 7.9 pKi = 7.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
44454060 155308 0 None - 1 Human 5.9 pKi = 5.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL403180 155308 0 None - 1 Human 5.9 pKi = 5.9 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
44454367 95232 0 None - 1 Human 7.8 pKi = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
CHEMBL256235 95232 0 None - 1 Human 7.8 pKi = 7.8 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
44454338 97807 0 None - 1 Human 6.7 pKi = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL272085 97807 0 None - 1 Human 6.7 pKi = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
44434080 89882 0 None - 1 Human 6.7 pKi = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL237933 89882 0 None - 1 Human 6.7 pKi = 6.7 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2008.01.100
44454302 159356 0 None - 1 Human 6.6 pKi = 6.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
CHEMBL410060 159356 0 None - 1 Human 6.6 pKi = 6.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
44454092 97621 0 None - 1 Human 5.6 pKi = 5.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
CHEMBL271082 97621 0 None - 1 Human 5.6 pKi = 5.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
44454432 155234 0 None - 1 Human 5.6 pKi = 5.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
CHEMBL402808 155234 0 None - 1 Human 5.6 pKi = 5.6 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
9950632 88677 0 None - 1 Human 5.5 pKi = 5.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.01.100
CHEMBL236038 88677 0 None - 1 Human 5.5 pKi = 5.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2008.01.100
44454399 155115 0 None - 1 Human 6.5 pKi = 6.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 447 11 2 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC(C#N)Cc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL402086 155115 0 None - 1 Human 6.5 pKi = 6.5 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 447 11 2 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC(C#N)Cc1ccccc1 10.1016/j.bmcl.2008.01.100
44454432 155234 0 None - 1 Human 5.4 pKi = 5.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
CHEMBL402808 155234 0 None - 1 Human 5.4 pKi = 5.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1 10.1016/j.bmcl.2008.01.100
25022640 97773 0 None - 1 Human 7.4 pKi = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
CHEMBL271876 97773 0 None - 1 Human 7.4 pKi = 7.4 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
44454092 97621 0 None - 1 Human 6.3 pKi = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
CHEMBL271082 97621 0 None - 1 Human 6.3 pKi = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1 10.1016/j.bmcl.2008.01.100
44454303 97541 0 None - 1 Human 8.2 pKi = 8.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
CHEMBL270666 97541 0 None - 1 Human 8.2 pKi = 8.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1O 10.1016/j.bmcl.2008.01.100
44454304 97575 0 None - 1 Human 6.3 pKi = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
CHEMBL270876 97575 0 None - 1 Human 6.3 pKi = 6.3 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccn1 10.1016/j.bmcl.2008.01.100
56926461 69007 0 None - 1 Human 8.2 pKi = 8.2 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm1012374
CHEMBL1923609 69007 0 None - 1 Human 8.2 pKi = 8.2 Functional
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm1012374
44454398 97570 0 None - 1 Human 6.2 pKi = 6.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 447 11 2 8 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(C#N)c1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL270851 97570 0 None - 1 Human 6.2 pKi = 6.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 447 11 2 8 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(C#N)c1ccccc1 10.1016/j.bmcl.2008.01.100
44454060 155308 0 None - 1 Human 7.2 pKi = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL403180 155308 0 None - 1 Human 7.2 pKi = 7.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1 10.1016/j.bmcl.2008.01.100
44454367 95232 0 None - 1 Human 6.2 pKi = 6.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
CHEMBL256235 95232 0 None - 1 Human 6.2 pKi = 6.2 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F 10.1016/j.bmcl.2008.01.100
44454337 155579 0 None - 1 Human 8.1 pKi = 8.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
CHEMBL404545 155579 0 None - 1 Human 8.1 pKi = 8.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1 10.1016/j.bmcl.2008.01.100
44454117 155532 0 None - 1 Human 6.1 pKi = 6.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
CHEMBL404336 155532 0 None - 1 Human 6.1 pKi = 6.1 Functional
Agonist activity at human GHS receptor expressed in H4 glioma cellsAgonist activity at human GHS receptor expressed in H4 glioma cells
ChEMBL 459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N 10.1016/j.bmcl.2008.01.100
1099 1773 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Measuring ghrelin-induced GHSR activation detected by β-arrestin recruitment in cells stably expressing hGHSR.Measuring ghrelin-induced GHSR activation detected by β-arrestin recruitment in cells stably expressing hGHSR.
Guide to Pharmacology None None None None 29233536
121879 2222 24 None -3 5 Human 7.0 pEC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 15905359
5868 2222 24 None -3 5 Human 7.0 pEC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 15905359
CHEMBL308716 2222 24 None -3 5 Human 7.0 pEC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 15905359
5869 4049 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21402696
121879 2222 24 None 1 5 Rat 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 8503009
5868 2222 24 None 1 5 Rat 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 8503009
CHEMBL308716 2222 24 None 1 5 Rat 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 8503009
1099 1773 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10628755
1099 1773 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
121879 2222 24 None -3 5 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 15905359
5868 2222 24 None -3 5 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 15905359
CHEMBL308716 2222 24 None -3 5 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 15905359
1093 1781 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
4345065 1781 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
1093 1781 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
4345065 1781 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
178024 1958 33 None -1 3 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10427162
178024 1958 33 None -1 3 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 15905359
5867 1958 33 None -1 3 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10427162
5867 1958 33 None -1 3 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 15905359
CHEMBL13817 1958 33 None -1 3 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10427162
CHEMBL13817 1958 33 None -1 3 Human 9.2 pEC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 15905359
1099 1773 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12907757
1099 1773 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21402696
5866 3597 4 None - 1 Human 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 18923064
9804743 3597 4 None - 1 Human 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 18923064
CHEMBL360227 3597 4 None - 1 Human 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 18923064
9734 2316 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
IC<sub>50</sub> for LEAP2 antagonism of GHSR activation in the presence of ghrelin.IC<sub>50</sub> for LEAP2 antagonism of GHSR activation in the presence of ghrelin.
Guide to Pharmacology None None None None 29233536
11441554 220 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 6 4 6 3.9 O=C(NC(C)(C)C)Nc1ccc(cc1)c1c(N)nc(nc1COCc1ccccc1)N 16854051
5871 220 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 6 4 6 3.9 O=C(NC(C)(C)C)Nc1ccc(cc1)c1c(N)nc(nc1COCc1ccccc1)N 16854051
CHEMBL212761 220 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 6 4 6 3.9 O=C(NC(C)(C)C)Nc1ccc(cc1)c1c(N)nc(nc1COCc1ccccc1)N 16854051
5872 2111 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 603 10 3 8 5.4 COc1ccc(c(c1)OC)n1c(nnc1n1cc(c2c1cccc2)CC)[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H]1CCCN1 17927165
74015851 2111 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 603 10 3 8 5.4 COc1ccc(c(c1)OC)n1c(nnc1n1cc(c2c1cccc2)CC)[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@@H]1CCCN1 17927165
25124566 1861 8 None 2 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 20593439
5870 1861 8 None 2 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 20593439
CHEMBL3358452 1861 8 None 2 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 20593439
5866 3597 4 None - 1 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 11741481
9804743 3597 4 None - 1 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 11741481
CHEMBL360227 3597 4 None - 1 Human 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 11741481
25124566 1861 8 None -2 2 Rat 8.0 pKB = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 21034740
5870 1861 8 None -2 2 Rat 8.0 pKB = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 21034740
CHEMBL3358452 1861 8 None -2 2 Rat 8.0 pKB = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 21034740




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
2713 205248 82 None - 0 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5353524 205248 82 None - 0 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5360566 205248 82 None - 0 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
88536661 205248 82 None - 0 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
9552079 205248 82 None - 0 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1330113 205248 82 None - 0 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL790 205248 82 None - 0 Human 6.0 pAC50 = 6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
156419 935 74 None - 1 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
3308 935 74 None - 1 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
647 935 74 None - 1 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL1201284 935 74 None - 1 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
DB01012 935 74 None - 1 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
5920 47245 83 None - 1 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 651 5 3 4 4.0 N[C@@H](Cc1cc(I)c(Oc2ccc(O)c(I)c2)c(I)c1)C(=O)O 10.1038/s41467-023-40064-9
7048703 47245 83 None - 1 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 651 5 3 4 4.0 N[C@@H](Cc1cc(I)c(Oc2ccc(O)c(I)c2)c(I)c1)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL1544 47245 83 None - 1 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 651 5 3 4 4.0 N[C@@H](Cc1cc(I)c(Oc2ccc(O)c(I)c2)c(I)c1)C(=O)O 10.1038/s41467-023-40064-9
148192 10388 81 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 704 14 5 9 4.2 COC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)[C@@H](O)CN(Cc1ccc(-c2ccccn2)cc1)NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)C(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL1163 10388 81 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 704 14 5 9 4.2 COC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)[C@@H](O)CN(Cc1ccc(-c2ccccn2)cc1)NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)C(C)(C)C 10.1038/s41467-023-40064-9
154257 178595 67 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
CHEMBL46740 178595 67 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
2600 3750 74 None - 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 3750 74 None - 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 3750 74 None - 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 3750 74 None - 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 3750 74 None - 13 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
47319 26433 35 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 929 24 0 12 8.1 COc1ccc(CC2c3cc(OC)c(OC)cc3CC[N+]2(C)CCC(=O)OCCCCCOC(=O)CC[N+]2(C)CCc3cc(OC)c(OC)cc3C2Cc2ccc(OC)c(OC)c2)cc1OC 10.1038/s41467-023-40064-9
CHEMBL1360 26433 35 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 929 24 0 12 8.1 COc1ccc(CC2c3cc(OC)c(OC)cc3CC[N+]2(C)CCC(=O)OCCCCCOC(=O)CC[N+]2(C)CCc3cc(OC)c(OC)cc3C2Cc2ccc(OC)c(OC)c2)cc1OC 10.1038/s41467-023-40064-9
135409453 3744 41 None - 2 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 3744 41 None - 2 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 3744 41 None - 2 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
71496458 115538 87 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
CHEMBL3353410 115538 87 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
242 469 124 None - 52 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 469 124 None - 52 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 469 124 None - 52 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 469 124 None - 52 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 469 124 None - 52 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
39186 85906 54 None - 2 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 414 6 0 6 3.4 COc1ccc([C@@H]2Sc3ccccc3N(CCN(C)C)C(=O)[C@@H]2OC(C)=O)cc1 10.1038/s41467-023-40064-9
CHEMBL23 85906 54 None - 2 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 414 6 0 6 3.4 COc1ccc([C@@H]2Sc3ccccc3N(CCN(C)C)C(=O)[C@@H]2OC(C)=O)cc1 10.1038/s41467-023-40064-9
16362 3103 71 None - 30 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2172 3103 71 None - 30 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
90 3103 71 None - 30 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1423 3103 71 None - 30 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01100 3103 71 None - 30 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
3042 1402 35 None - 15 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
355 1402 35 None - 15 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
868 1402 35 None - 15 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
CHEMBL1123 1402 35 None - 15 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
DB00804 1402 35 None - 15 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 309 7 0 3 4.4 CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC 10.1038/s41467-023-40064-9
10184665 3960 51 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
4799 3960 51 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
7353 3960 51 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
CHEMBL1198857 3960 51 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
DB09082 3960 51 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
3191 102831 97 None - 25 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
CHEMBL305660 102831 97 None - 25 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
3926 207218 40 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 491 9 1 3 5.8 Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL92870 207218 40 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 491 9 1 3 5.8 Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
11626560 200914 94 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
CHEMBL601719 200914 94 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
2267 557 71 None - 7 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
271 557 71 None - 7 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
7121 557 71 None - 7 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL639 557 71 None - 7 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
DB00972 557 71 None - 7 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
135564886 14461 5 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
135673376 14461 5 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
137157436 14461 5 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
145948239 14461 5 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
71587099 14461 5 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
CHEMBL1201304 14461 5 None - 0 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 752 14 1 6 8.7 CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21 10.1038/s41467-023-40064-9
2585 800 103 None - 22 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
522 800 103 None - 22 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
551 800 103 None - 22 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
CHEMBL723 800 103 None - 22 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
DB01136 800 103 None - 22 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
1353 1898 93 None - 86 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 1898 93 None - 86 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 1898 93 None - 86 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 1898 93 None - 86 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 1898 93 None - 86 Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
100 3776 58 None - 56 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
2637 3776 58 None - 56 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
5452 3776 58 None - 56 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
CHEMBL479 3776 58 None - 56 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
DB00679 3776 58 None - 56 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
202 1496 77 None - 33 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
60835 1496 77 None - 33 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
972 1496 77 None - 33 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1175 1496 77 None - 33 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
DB00476 1496 77 None - 33 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
11976 917 59 None - 24 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
667467 917 59 None - 24 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
CHEMBL908 917 59 None - 24 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
DB01239 917 59 None - 24 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
2218 15251 23 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 322 8 0 2 4.4 CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1 10.1038/s41467-023-40064-9
CHEMBL1213033 15251 23 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 322 8 0 2 4.4 CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1 10.1038/s41467-023-40064-9
41684 31191 105 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
CHEMBL1401 31191 105 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
3025 7243 86 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 10 1 4 3.5 CCCCOc1cc(C(=O)NCCN(CC)CC)c2ccccc2n1 10.1038/s41467-023-40064-9
CHEMBL1086 7243 86 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 10 1 4 3.5 CCCCOc1cc(C(=O)NCCN(CC)CC)c2ccccc2n1 10.1038/s41467-023-40064-9
44112 121264 48 None - 7 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 10.1038/s41467-023-40064-9
CHEMBL357995 121264 48 None - 7 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 380 7 2 4 4.5 Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1 10.1038/s41467-023-40064-9
68617 205504 62 None - 26 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1709 205504 62 None - 26 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL809 205504 62 None - 26 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
2726 916 68 None - 73 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 916 68 None - 73 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 916 68 None - 73 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 916 68 None - 73 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 916 68 None - 73 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
16363 593 53 None - 7 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
312 593 53 None - 7 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
9215 593 53 None - 7 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL297302 593 53 None - 7 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB12867 593 53 None - 7 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2291 3162 58 None - 12 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
2561 3162 58 None - 12 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
4932 3162 58 None - 12 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL631 3162 58 None - 12 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
DB01182 3162 58 None - 12 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
24826799 10766 104 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 532 4 1 6 4.5 Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12 10.1038/s41467-023-40064-9
CHEMBL1171837 10766 104 None - 0 Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 532 4 1 6 4.5 Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12 10.1038/s41467-023-40064-9
2274 3151 58 None - 32 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4917 3151 58 None - 32 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
7279 3151 58 None - 32 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL728 3151 58 None - 32 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00433 3151 58 None - 32 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
2398 951 62 None - 29 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801 951 62 None - 29 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
701 951 62 None - 29 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL415 951 62 None - 29 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB01242 951 62 None - 29 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
4046 2466 33 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4252 2466 33 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
CHEMBL416956 2466 33 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
DB00358 2466 33 None - 2 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
3074 17926 26 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 604 16 0 12 3.5 COc1cc(C(=O)OCCCN2CCCN(CCCOC(=O)c3cc(OC)c(OC)c(OC)c3)CC2)cc(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL126075 17926 26 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 604 16 0 12 3.5 COc1cc(C(=O)OCCCN2CCCN(CCCOC(=O)c3cc(OC)c(OC)c(OC)c3)CC2)cc(OC)c1OC 10.1038/s41467-023-40064-9
4413 98045 57 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 347 4 5 4 2.6 N=C(N)Nc1ccc(C(=O)Oc2ccc3cc(C(=N)N)ccc3c2)cc1 10.1038/s41467-023-40064-9
CHEMBL273264 98045 57 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 347 4 5 4 2.6 N=C(N)Nc1ccc(C(=O)Oc2ccc3cc(C(=N)N)ccc3c2)cc1 10.1038/s41467-023-40064-9
25382 9125 37 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL110094 9125 37 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
2375 158370 106 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 430 5 2 5 2.9 CC(O)(CS(=O)(=O)c1ccc(F)cc1)C(=O)Nc1ccc(C#N)c(C(F)(F)F)c1 10.1038/s41467-023-40064-9
CHEMBL409 158370 106 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 430 5 2 5 2.9 CC(O)(CS(=O)(=O)c1ccc(F)cc1)C(=O)Nc1ccc(C#N)c(C(F)(F)F)c1 10.1038/s41467-023-40064-9
2351 4269 49 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1008 4269 49 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1257078 4269 49 None - 0 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
448537 160226 89 None - 25 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL411 160226 89 None - 25 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 10.1038/s41467-023-40064-9
3393 207901 24 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 387 6 0 3 4.0 CCN(CC)CCN1C(=O)CN=C(c2ccccc2F)c2cc(Cl)ccc21 10.1038/s41467-023-40064-9
CHEMBL968 207901 24 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 387 6 0 3 4.0 CCN(CC)CCN1C(=O)CN=C(c2ccccc2F)c2cc(Cl)ccc21 10.1038/s41467-023-40064-9
441243 9804 58 None - 8 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 670 12 5 7 3.1 CC(C)(C)NC(=O)[C@@H]1C[C@@H]2CCCC[C@@H]2CN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)c1ccc2ccccc2n1 10.1038/s41467-023-40064-9
CHEMBL114 9804 58 None - 8 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 670 12 5 7 3.1 CC(C)(C)NC(=O)[C@@H]1C[C@@H]2CCCC[C@@H]2CN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)c1ccc2ccccc2n1 10.1038/s41467-023-40064-9
214 3831 58 None - 30 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 3831 58 None - 30 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 3831 58 None - 30 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 3831 58 None - 30 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 3831 58 None - 30 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 3831 58 None - 30 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
46780481 107504 20 None - 54 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
9903970 107504 20 None - 54 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3187365 107504 20 None - 54 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3544974 107504 20 None - 54 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
6436173 55086 45 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL1617 55086 45 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
8550 14392 57 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 578 7 1 9 4.2 COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5ccccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC 10.1038/s41467-023-40064-9
CHEMBL1200515 14392 57 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 578 7 1 9 4.2 COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5ccccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC 10.1038/s41467-023-40064-9
31101 726 40 None - 36 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
35 726 40 None - 36 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
403 726 40 None - 36 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
CHEMBL493 726 40 None - 36 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
DB01200 726 40 None - 36 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
104850 3305 96 None - 6 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
4150 3305 96 None - 6 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
743 3305 96 None - 6 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL111 3305 96 None - 6 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
DB06155 3305 96 None - 6 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
392622 56282 95 None - 4 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
CHEMBL163 56282 95 None - 4 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
2995 204382 53 None - 23 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1696 204382 53 None - 23 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL72 204382 53 None - 23 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
3947 206372 53 None - 16 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL87708 206372 53 None - 16 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
212 3777 47 None - 25 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2639 3777 47 None - 25 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651 3777 47 None - 25 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL1201 3777 47 None - 25 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01623 3777 47 None - 25 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL3039583 210926 0 None - 0 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](c2ccccc2)NC(=O)[C@@H]2C[C@H](OC(=O)NCCN)CN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(OCc3ccccc3)cc2)NC1=O 10.1038/s41467-023-40064-9
60065 84340 6 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 505 7 1 8 4.2 COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@@H]2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL2218858 84340 6 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 505 7 1 8 4.2 COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@@H]2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
3081361 93905 123 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
CHEMBL24828 93905 123 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
107771 120222 49 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 517 7 2 7 6.1 COc1ccc2nc3cc(Cl)ccc3c(Nc3cc(CN4CCCC4)c(O)c(CN4CCCC4)c3)c2n1 10.1038/s41467-023-40064-9
CHEMBL35228 120222 49 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 517 7 2 7 6.1 COc1ccc2nc3cc(Cl)ccc3c(Nc3cc(CN4CCCC4)c(O)c(CN4CCCC4)c3)c2n1 10.1038/s41467-023-40064-9
3151 1450 97 None - 27 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
945 1450 97 None - 27 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
965 1450 97 None - 27 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL219916 1450 97 None - 27 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01184 1450 97 None - 27 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
3949 100586 50 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 468 8 0 5 4.9 COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL29188 100586 50 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 468 8 0 5 4.9 COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC 10.1038/s41467-023-40064-9
2435 3563 83 None - 49 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
60149 3563 83 None - 49 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
98 3563 83 None - 49 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
CHEMBL12713 3563 83 None - 49 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
DB06144 3563 83 None - 49 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
25181577 78190 56 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 574 9 2 9 5.0 CCOC(=O)[C@@H](N)Cc1ccc(-c2cc(O[C@H](c3ccc(Cl)cc3-n3ccc(C)n3)C(F)(F)F)nc(N)n2)cc1 10.1038/s41467-023-40064-9
CHEMBL2105695 78190 56 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 574 9 2 9 5.0 CCOC(=O)[C@@H](N)Cc1ccc(-c2cc(O[C@H](c3ccc(Cl)cc3-n3ccc(C)n3)C(F)(F)F)nc(N)n2)cc1 10.1038/s41467-023-40064-9
2318 154832 29 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 351 7 1 3 4.1 CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL400599 154832 29 None - 0 Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 351 7 1 3 4.1 CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1 10.1038/s41467-023-40064-9
2407 3347 76 None - 7 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
59227 3347 76 None - 7 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
941 3347 76 None - 7 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
CHEMBL1303 3347 76 None - 7 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
DB05271 3347 76 None - 7 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
3380 22758 34 None - 1 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 2 0 4 2.5 CN1C(=O)CN=C(c2ccccc2F)c2cc([N+](=O)[O-])ccc21 10.1038/s41467-023-40064-9
CHEMBL13280 22758 34 None - 1 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 2 0 4 2.5 CN1C(=O)CN=C(c2ccccc2F)c2cc([N+](=O)[O-])ccc21 10.1038/s41467-023-40064-9
2202 3110 96 None - 21 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
4850 3110 96 None - 21 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
49 3110 96 None - 21 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
CHEMBL1371770 3110 96 None - 21 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
DB12478 3110 96 None - 21 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
4495 196512 92 None - 30 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL56367 196512 92 None - 30 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 10.1038/s41467-023-40064-9
9801 91556 35 None - 0 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 329 8 1 1 5.4 CC(Cc1ccccc1)NCCC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL24072 91556 35 None - 0 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 329 8 1 1 5.4 CC(Cc1ccccc1)NCCC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
6729 14453 41 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 432 5 0 2 6.5 CC(C)(C)c1ccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)cc1 10.1038/s41467-023-40064-9
CHEMBL1201271 14453 41 None - 0 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 432 5 0 2 6.5 CC(C)(C)c1ccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)cc1 10.1038/s41467-023-40064-9
1016 3720 78 None - 35 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
2561 3720 78 None - 35 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
2733526 3720 78 None - 35 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
5384 3720 78 None - 35 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL83 3720 78 None - 35 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
DB00675 3720 78 None - 35 Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 10.1038/s41467-023-40064-9
9915743 63512 93 None - 0 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 556 11 2 8 5.9 CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)/C=C/CN(C)C 10.1038/s41467-023-40064-9
CHEMBL180022 63512 93 None - 0 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 556 11 2 8 5.9 CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)/C=C/CN(C)C 10.1038/s41467-023-40064-9
275196 125647 52 None - 0 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 4 0 8 2.9 COc1ccc2c(c1OC)C(=O)O[C@@H]2[C@H]1c2c(cc3c(c2OC)OCO3)CCN1C 10.1038/s41467-023-40064-9
CHEMBL364713 125647 52 None - 0 Human 6.5 pAC50 = 6.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 4 0 8 2.9 COc1ccc2c(c1OC)C(=O)O[C@@H]2[C@H]1c2c(cc3c(c2OC)OCO3)CCN1C 10.1038/s41467-023-40064-9
26987 946 33 None - 21 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
6063 946 33 None - 21 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
671 946 33 None - 21 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
CHEMBL1626 946 33 None - 21 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
DB00283 946 33 None - 21 Human 5.5 pAC50 = 5.5 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C 10.1038/s41467-023-40064-9
11980903 14460 19 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
22526 14460 19 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
5281035 14460 19 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201303 14460 19 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
25077405 2696 0 None - 1 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
3902 2696 0 None - 1 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
CHEMBL1201309 2696 0 None - 1 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
DB00666 2696 0 None - 1 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL None None None None 10.1038/s41467-023-40064-9
102 4096 48 None - 50 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
3659 4096 48 None - 50 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
8969 4096 48 None - 50 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL15245 4096 48 None - 50 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
DB01392 4096 48 None - 50 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
4034 55792 55 None - 1 Human 4.4 pAC50 = 4.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
CHEMBL1623 55792 55 None - 1 Human 4.4 pAC50 = 4.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
5328940 100188 107 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
CHEMBL288441 100188 107 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
10531 1408 21 None - 24 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
121 1408 21 None - 24 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
888 1408 21 None - 24 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
CHEMBL1732 1408 21 None - 24 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
DB00320 1408 21 None - 24 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
118422671 2737 65 None - 4 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
1887 2737 65 None - 4 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
71301 2737 65 None - 4 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
7246 2737 65 None - 4 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL434394 2737 65 None - 4 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
DB04861 2737 65 None - 4 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
30323 62455 57 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL1563 62455 57 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL178 62455 57 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 527 4 5 11 1.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(C)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
10096344 89565 85 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 472 4 1 10 1.1 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(Cc1nc(C)c3ccccc3n1)c(=O)n2C 10.1038/s41467-023-40064-9
CHEMBL237500 89565 85 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 472 4 1 10 1.1 CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(Cc1nc(C)c3ccccc3n1)c(=O)n2C 10.1038/s41467-023-40064-9
216416 111554 48 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL328190 111554 48 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
319 1312 44 None - 9 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
321 1312 44 None - 9 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
444031 1312 44 None - 9 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
784 1312 44 None - 9 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
CHEMBL1346 1312 44 None - 9 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
DB00496 1312 44 None - 9 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1038/s41467-023-40064-9
3149 12582 15 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1187011 12582 15 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
4746 204868 31 None - 4 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL1334033 204868 31 None - 4 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
CHEMBL75880 204868 31 None - 4 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 277 4 1 1 5.3 C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1 10.1038/s41467-023-40064-9
2335 11816 22 None - 12 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
8478 11816 22 None - 12 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 11816 22 None - 12 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL221753 11816 22 None - 12 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
65709 59851 39 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 365 8 0 5 3.3 CCN(CC)CCn1c(=O)c(Cc2ccc(OC)cc2)nc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1729803 59851 39 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 365 8 0 5 3.3 CCN(CC)CCn1c(=O)c(Cc2ccc(OC)cc2)nc2ccccc21 10.1038/s41467-023-40064-9
11643449 89926 3 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 753 6 5 10 2.7 CC[C@]1(O)C[C@@H]2CN(CCc3c([nH]c4ccccc34)[C@@](C(=O)OC)(c3cc4c(cc3OC)N(C)[C@H]3[C@@](O)(C(N)=O)[C@H](O)[C@]5(CC)C=CCN6CC[C@]43[C@@H]65)C2)C1 10.1038/s41467-023-40064-9
CHEMBL238071 89926 3 None - 0 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 753 6 5 10 2.7 CC[C@]1(O)C[C@@H]2CN(CCc3c([nH]c4ccccc34)[C@@](C(=O)OC)(c3cc4c(cc3OC)N(C)[C@H]3[C@@](O)(C(N)=O)[C@H](O)[C@]5(CC)C=CCN6CC[C@]43[C@@H]65)C2)C1 10.1038/s41467-023-40064-9
2448 99295 70 None - 18 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
CHEMBL28218 99295 70 None - 18 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
4452 2742 19 None - 19 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
983 2742 19 None - 19 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
CHEMBL20734 2742 19 None - 19 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
176 397 66 None - 31 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2157 397 66 None - 31 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2566 397 66 None - 31 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
CHEMBL633 397 66 None - 31 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
DB01118 397 66 None - 31 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
1222 1651 49 None - 33 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3396 1651 49 None - 33 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
85 1651 49 None - 33 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL46516 1651 49 None - 33 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
DB04842 1651 49 None - 33 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
5329102 194703 86 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 194703 86 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
72093 35031 9 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL1433361 35031 9 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL2103773 35031 9 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
42890 9393 59 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 497 3 5 10 1.0 CC(=O)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
CHEMBL1117 9393 59 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 497 3 5 10 1.0 CC(=O)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
1164 1617 26 None - 12 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
1626 1617 26 None - 12 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
3345 1617 26 None - 12 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL596 1617 26 None - 12 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
DB00813 1617 26 None - 12 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1038/s41467-023-40064-9
2247 504 81 None - 42 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 504 81 None - 42 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 504 81 None - 42 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 504 81 None - 42 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 504 81 None - 42 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
5482 14388 80 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 386 6 0 4 5.9 Clc1ccc(C(Cn2ccnc2)OCc2ccsc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1200438 14388 80 None - 0 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 386 6 0 4 5.9 Clc1ccc(C(Cn2ccnc2)OCc2ccsc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
1385580 29245 76 None - 5 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
4615 29245 76 None - 5 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL13828 29245 76 None - 5 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
16722836 18953 99 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 524 10 3 8 4.8 Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1 10.1038/s41467-023-40064-9
CHEMBL1287853 18953 99 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 524 10 3 8 4.8 Cc1cnc(Nc2ccc(OCCN3CCCC3)cc2)nc1Nc1cccc(S(=O)(=O)NC(C)(C)C)c1 10.1038/s41467-023-40064-9
2794 19348 85 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 472 4 1 4 7.5 CC(C)/N=c1\cc2n(-c3ccc(Cl)cc3)c3ccccc3nc-2cc1Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1292 19348 85 None - 0 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 472 4 1 4 7.5 CC(C)/N=c1\cc2n(-c3ccc(Cl)cc3)c3ccccc3nc-2cc1Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
3883 183511 112 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 369 5 1 4 3.5 Cc1c(OCC(F)(F)F)ccnc1C[S+]([O-])c1nc2ccccc2[nH]1 10.1038/s41467-023-40064-9
CHEMBL480 183511 112 None - 0 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GHSR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 369 5 1 4 3.5 Cc1c(OCC(F)(F)F)ccnc1C[S+]([O-])c1nc2ccccc2[nH]1 10.1038/s41467-023-40064-9
178024 1958 33 None - 1 Human 9.7 pEC50 = 9.7 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm301653f
5867 1958 33 None - 1 Human 9.7 pEC50 = 9.7 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm301653f
CHEMBL13817 1958 33 None - 1 Human 9.7 pEC50 = 9.7 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm301653f
22867441 10283 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
CHEMBL1161835 10283 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
67457995 91804 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@H](O)c1ccccc12 10.1016/j.bmc.2013.06.006
CHEMBL2413152 91804 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@H](O)c1ccccc12 10.1016/j.bmc.2013.06.006
22867441 10283 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
CHEMBL1161835 10283 0 None - 0 Human 9.2 pEC50 = 9.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 474 5 4 4 2.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
71716660 85973 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 5 5 2.7 CCNC(O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
CHEMBL2304221 85973 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 5 5 2.7 CCNC(O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
10345516 139250 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1021/jm058053k
CHEMBL379074 139250 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1021/jm058053k
71716660 85973 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 5 5 2.7 CCNC(O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
CHEMBL2304221 85973 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 5 5 2.7 CCNC(O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
10345516 139250 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1021/jm058053k
CHEMBL379074 139250 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1 10.1021/jm058053k
9807597 182993 5 None - 0 Human 9.0 pEC50 = 9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 513 7 4 4 3.5 CNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1021/jm058053k
CHEMBL47938 182993 5 None - 0 Human 9.0 pEC50 = 9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 513 7 4 4 3.5 CNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1021/jm058053k
10323604 10277 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161828 10277 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
10323604 10277 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161828 10277 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
44411920 77849 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 3 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
CHEMBL209360 77849 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 3 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
162662316 181499 0 None - 0 Rat 8.9 pEC50 = 8.9 Binding
Agonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIAAgonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIA
ChEMBL 542 8 3 6 2.6 CC(C)(N)NC(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CC(S(C)(=O)=O)c1ccccc12 10.1021/acs.jmedchem.0c00829
CHEMBL4765101 181499 0 None - 0 Rat 8.9 pEC50 = 8.9 Binding
Agonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIAAgonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIA
ChEMBL 542 8 3 6 2.6 CC(C)(N)NC(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CC(S(C)(=O)=O)c1ccccc12 10.1021/acs.jmedchem.0c00829
90666017 109273 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at GSH-R1a in human U2OS cells after 2 hrs by FLIPR assayAgonist activity at GSH-R1a in human U2OS cells after 2 hrs by FLIPR assay
ChEMBL 472 6 0 8 4.1 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218890 109273 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at GSH-R1a in human U2OS cells after 2 hrs by FLIPR assayAgonist activity at GSH-R1a in human U2OS cells after 2 hrs by FLIPR assay
ChEMBL 472 6 0 8 4.1 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
44411920 77849 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 3 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
CHEMBL209360 77849 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 3 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12 10.1021/jm058053k
10625750 168130 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
CHEMBL433087 168130 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
10625750 168130 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
CHEMBL433087 168130 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 518 9 3 5 3.3 CCOC(=O)[C@@]1(Cc2ccccc2)CCCN(C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)C1 10.1021/jm058053k
10626337 101198 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1021/jm058053k
CHEMBL295984 101198 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1021/jm058053k
44411718 10274 0 None - 0 Human 8.0 pEC50 = 8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 467 7 2 5 3.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161825 10274 0 None - 0 Human 8.0 pEC50 = 8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 467 7 2 5 3.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
44293557 101061 0 None - 0 Human 8.0 pEC50 = 8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL294923 101061 0 None - 0 Human 8.0 pEC50 = 8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL540001 101061 0 None - 0 Human 8.0 pEC50 = 8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
16040587 179360 0 None - 0 Human 7.0 pEC50 = 7 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1 10.1021/jm301653f
CHEMBL473921 179360 0 None - 0 Human 7.0 pEC50 = 7 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1 10.1021/jm301653f
16040587 179360 0 None - 0 Human 7.0 pEC50 = 7 Binding
Inhibition of human Ghrelin receptorInhibition of human Ghrelin receptor
ChEMBL 501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1 10.1016/j.bmcl.2008.10.072
CHEMBL473921 179360 0 None - 0 Human 7.0 pEC50 = 7 Binding
Inhibition of human Ghrelin receptorInhibition of human Ghrelin receptor
ChEMBL 501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1 10.1016/j.bmcl.2008.10.072
16752689 188344 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 568 10 2 4 6.6 COc1cccc(CCN(Cc2ccccc2-c2ccc(CN3C[C@H](C)N[C@H](C)C3)cc2)C(=O)NC2CCCCC2)c1 10.1021/jm301653f
CHEMBL501315 188344 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
ChEMBL 568 10 2 4 6.6 COc1cccc(CCN(Cc2ccccc2-c2ccc(CN3C[C@H](C)N[C@H](C)C3)cc2)C(=O)NC2CCCCC2)c1 10.1021/jm301653f
9890375 98242 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL274599 98242 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL558802 98242 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
9890375 98242 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL274599 98242 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL558802 98242 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
10026738 162745 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL417182 162745 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL557206 162745 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
10026738 162745 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL417182 162745 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL557206 162745 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
10745533 140095 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL380096 140095 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
10745533 140095 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL380096 140095 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
44411745 10276 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
CHEMBL1161827 10276 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
10626337 101198 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1021/jm058053k
CHEMBL295984 101198 0 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O 10.1021/jm058053k
44411634 10273 1 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161824 10273 1 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
44411634 10273 1 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161824 10273 1 None - 0 Human 8.7 pEC50 = 8.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
44411745 10276 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
CHEMBL1161827 10276 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
44411753 10278 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
CHEMBL1161829 10278 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
44411753 10278 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
CHEMBL1161829 10278 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
44293091 188162 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL49884 188162 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
44293091 188162 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
CHEMBL49884 188162 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm058053k
46905972 10377 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 471 10 1 3 4.8 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)Cc1ccccc1 10.1021/jm058053k
CHEMBL1162926 10377 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 471 10 1 3 4.8 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)Cc1ccccc1 10.1021/jm058053k
15481181 77715 2 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
CHEMBL209020 77715 2 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
9810101 99221 17 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL281764 99221 17 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
15481188 141185 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1021/jm058053k
CHEMBL382844 141185 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1021/jm058053k
CHEMBL1793862 208905 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL None None None CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm058053k
216208 9695 33 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIAAgonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIA
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.0c00829
CHEMBL113313 9695 33 None - 1 Rat 8.5 pEC50 = 8.5 Binding
Agonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIAAgonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIA
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.0c00829
46905972 10377 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 471 10 1 3 4.8 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)Cc1ccccc1 10.1021/jm058053k
CHEMBL1162926 10377 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 471 10 1 3 4.8 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)Cc1ccccc1 10.1021/jm058053k
15481181 77715 2 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
CHEMBL209020 77715 2 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
9810101 99221 17 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL281764 99221 17 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
15481188 141185 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1021/jm058053k
CHEMBL382844 141185 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1 10.1021/jm058053k
CHEMBL1793862 208905 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL None None None CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm058053k
15481185 77232 1 None - 0 Human 8.4 pEC50 = 8.4 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
CHEMBL207970 77232 1 None - 0 Human 8.4 pEC50 = 8.4 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
15481185 77232 1 None - 0 Human 8.4 pEC50 = 8.4 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
CHEMBL207970 77232 1 None - 0 Human 8.4 pEC50 = 8.4 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O 10.1021/jm058053k
44411584 10271 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161822 10271 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
44411584 10271 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161822 10271 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 465 7 2 4 3.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
22862436 10282 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161834 10282 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
10602640 138164 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1021/jm058053k
CHEMBL376970 138164 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1021/jm058053k
10791616 139511 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL379564 139511 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
10029990 169260 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL441360 169260 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
22862436 10282 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161834 10282 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 499 7 2 6 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
10602640 138164 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1021/jm058053k
CHEMBL376970 138164 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 545 14 2 5 4.2 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1OCCO 10.1021/jm058053k
10791616 139511 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL379564 139511 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 503 11 1 4 5.2 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
10029990 169260 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL441360 169260 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 531 13 2 5 4.0 CN(CCc1ccccc1OCCO)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
44411632 10272 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161823 10272 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
44411632 10272 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161823 10272 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 476 5 3 4 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
23529194 102164 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
Agonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIAAgonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIA
ChEMBL 525 5 3 3 4.0 O=C(NC(Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1)NC1CN2CCC1CC2 10.1021/acs.jmedchem.0c00829
CHEMBL302810 102164 0 None - 0 Rat 7.3 pEC50 = 7.3 Binding
Agonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIAAgonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIA
ChEMBL 525 5 3 3 4.0 O=C(NC(Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1)NC1CN2CCC1CC2 10.1021/acs.jmedchem.0c00829
16041292 183587 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Inhibition of human Ghrelin receptorInhibition of human Ghrelin receptor
ChEMBL 490 6 2 6 3.9 C[C@H]1CN(Cc2ccc(-n3ccnc3C(=O)N3CCC(Nc4cccc(F)c4)CC3)cc2)C[C@@H](C)N1 10.1016/j.bmcl.2008.10.072
CHEMBL480219 183587 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Inhibition of human Ghrelin receptorInhibition of human Ghrelin receptor
ChEMBL 490 6 2 6 3.9 C[C@H]1CN(Cc2ccc(-n3ccnc3C(=O)N3CCC(Nc4cccc(F)c4)CC3)cc2)C[C@@H](C)N1 10.1016/j.bmcl.2008.10.072
44411913 10281 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161833 10281 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
44411913 10281 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
CHEMBL1161833 10281 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 6 2 4 3.5 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12 10.1021/jm058053k
44411905 10280 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161832 10280 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
10506325 101214 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1021/jm058053k
CHEMBL296104 101214 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1021/jm058053k
44411905 10280 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
CHEMBL1161832 10280 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 6 2 5 2.2 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12 10.1021/jm058053k
10506325 101214 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1021/jm058053k
CHEMBL296104 101214 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 527 8 4 4 3.9 CCNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1 10.1021/jm058053k
10600702 141311 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL383526 141311 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
10600702 141311 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL383526 141311 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 477 10 1 4 4.7 CN(CCc1cccs1)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N 10.1021/jm058053k
CHEMBL335799 211541 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmc.2013.06.006
44411720 10275 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
CHEMBL1161826 10275 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
44411902 10279 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
CHEMBL1161831 10279 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
44411720 10275 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
CHEMBL1161826 10275 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 483 7 2 5 2.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12 10.1021/jm058053k
44411902 10279 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
CHEMBL1161831 10279 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
ChEMBL 451 7 2 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12 10.1021/jm058053k
44390849 62885 0 None - 0 Human 10.7 pIC50 = 10.7 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc(Cl)cc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL178475 62885 0 None - 0 Human 10.7 pIC50 = 10.7 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc(Cl)cc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
25227441 113416 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 563 8 2 8 3.9 CCc1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
CHEMBL3319217 113416 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 563 8 2 8 3.9 CCc1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
CHEMBL501253 214110 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](COC(=O)CCCCCCCBr)NC(=O)[C@H](CO)NC(=O)CN)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm0001727
44582528 193392 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 3419 113 48 48 -14.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](COC(=O)CC12CC3CC(CC(C3)C1)C2)NC(=O)[C@H](CO)NC(=O)CN)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm0001727
91935097 193392 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 3419 113 48 48 -14.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](COC(=O)CC12CC3CC(CC(C3)C1)C2)NC(=O)[C@H](CO)NC(=O)CN)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm0001727
CHEMBL525994 193392 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 3419 113 48 48 -14.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](COC(=O)CC12CC3CC(CC(C3)C1)C2)NC(=O)[C@H](CO)NC(=O)CN)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O 10.1021/jm0001727
CHEMBL2310891 209472 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C(C)C 10.1021/jm0001727
90665845 109245 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 485 5 0 4 6.8 Cc1ccccc1-c1nc2ccc(-c3ccc(Cl)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218645 109245 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 485 5 0 4 6.8 Cc1ccccc1-c1nc2ccc(-c3ccc(Cl)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL500468 214092 0 None - 1 Human 9.9 pIC50 = 9.9 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/j.bmcl.2005.02.042
57422686 113420 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 600 8 2 9 4.1 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccc5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319221 113420 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 600 8 2 9 4.1 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccc5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL2310888 209470 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(N)=O)C(C)C 10.1021/jm0001727
11340044 141310 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(NCc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL383522 141310 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(NCc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
44336274 108543 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration (biotinylated probe) is evaluated for [35S]- MK-0677 bindingInhibitory concentration (biotinylated probe) is evaluated for [35S]- MK-0677 binding
ChEMBL 896 22 6 10 2.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CN(S(=O)(=O)CC(=O)NCCCCCCNC(=O)CCCC[C@@H]1SCC3NC(=O)NC31)c1ccccc12 10.1021/jm970342o
CHEMBL320289 108543 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration (biotinylated probe) is evaluated for [35S]- MK-0677 bindingInhibitory concentration (biotinylated probe) is evaluated for [35S]- MK-0677 binding
ChEMBL 896 22 6 10 2.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CN(S(=O)(=O)CC(=O)NCCCCCCNC(=O)CCCC[C@@H]1SCC3NC(=O)NC31)c1ccccc12 10.1021/jm970342o
122180027 121562 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 566 8 2 7 5.2 CC(C)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586033 121562 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 566 8 2 7 5.2 CC(C)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
118709502 113445 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 629 8 2 10 3.8 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)c(C#N)cc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319398 113445 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 629 8 2 10 3.8 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)c(C#N)cc4Cl)sc3c2)CC1 10.1021/jm500610n
44390862 63837 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2cc(Cl)ccc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL180349 63837 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2cc(Cl)ccc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
16133832 213308 18 None - 1 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm0001727
CHEMBL425281 213308 18 None - 1 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm0001727
CHEMBL500468 214092 0 None - 1 Human 9.6 pIC50 = 9.6 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1016/s0960-894x(01)00324-9
90665847 109247 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 475 5 0 6 5.3 Cc1ccccc1-c1nc2cn(-c3ccc(Cl)cc3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218647 109247 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 475 5 0 6 5.3 Cc1ccccc1-c1nc2cn(-c3ccc(Cl)cc3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
122182190 121983 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
CHEMBL3593815 121983 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
57422687 113421 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 604 8 2 9 3.9 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319222 113421 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 604 8 2 9 3.9 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
16114292 96905 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL266063 96905 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
16114292 96905 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
CHEMBL266063 96905 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
11225576 166013 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL425594 166013 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
122182047 121976 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593636 121976 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
11225576 166013 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL425594 166013 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 489 9 3 8 4.0 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
25260749 113419 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 579 9 2 9 3.7 CCOc1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
CHEMBL3319220 113419 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 579 9 2 9 3.7 CCOc1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
57422792 113444 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 635 8 2 10 4.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)c(Cl)cc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319397 113444 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 635 8 2 10 4.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)c(Cl)cc4Cl)sc3c2)CC1 10.1021/jm500610n
57422692 113418 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 575 8 2 8 4.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(C5CC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319219 113418 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 575 8 2 8 4.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(C5CC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL500468 214092 0 None - 1 Human 9.4 pIC50 = 9.4 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1021/jm020985q
122182043 121972 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 580 7 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593632 121972 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 580 7 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
118709506 113455 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 586 5 2 9 4.3 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)c(C#N)cc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319407 113455 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 586 5 2 9 4.3 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)c(C#N)cc4Cl)sc3c2)CC1 10.1021/jm500610n
178024 1958 33 None - 1 Human 9.4 pIC50 = 9.4 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm0309452
5867 1958 33 None - 1 Human 9.4 pIC50 = 9.4 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm0309452
CHEMBL13817 1958 33 None - 1 Human 9.4 pIC50 = 9.4 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm0309452
11431274 77315 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 467 9 3 8 3.8 CC(C)=CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL208424 77315 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 467 9 3 8 3.8 CC(C)=CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11410373 138510 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 558 10 4 8 4.2 Cc1cc(C)cc(CNC(=O)CCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)c1 10.1016/j.bmcl.2006.01.012
CHEMBL377514 138510 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 558 10 4 8 4.2 Cc1cc(C)cc(CNC(=O)CCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)c1 10.1016/j.bmcl.2006.01.012
44582531 188698 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 3368 117 49 47 -15.3 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm0001727
91935100 188698 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 3368 117 49 47 -15.3 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm0001727
CHEMBL504776 188698 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 3368 117 49 47 -15.3 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm0001727
122182046 121975 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 586 8 2 6 5.6 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCC3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593635 121975 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 586 8 2 6 5.6 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCC3)cc1Cl 10.1016/j.bmc.2015.05.047
25260745 113448 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 573 10 2 8 5.2 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(-n4cccc4)ccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319400 113448 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 573 10 2 8 5.2 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(-n4cccc4)ccc3Cl)sc2c1 10.1021/jm500610n
122182190 121983 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
CHEMBL3593815 121983 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
57422768 113427 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 615 8 2 10 3.8 Cc1ccn(-c2ccc(C(=O)NC(=O)Nc3nc4ccc(S(=O)(=O)CCCN5CCN(C)CC5)cc4s3)c(Cl)c2)n1 10.1021/jm500610n
CHEMBL3319228 113427 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 615 8 2 10 3.8 Cc1ccn(-c2ccc(C(=O)NC(=O)Nc3nc4ccc(S(=O)(=O)CCCN5CCN(C)CC5)cc4s3)c(Cl)c2)n1 10.1021/jm500610n
16114096 79131 1 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)c(OC)c1 10.1021/jm0704550
CHEMBL2113324 79131 1 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)c(OC)c1 10.1021/jm0704550
178024 1958 33 None - 1 Human 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cellsAbility to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cells
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020424z
5867 1958 33 None - 1 Human 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cellsAbility to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cells
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020424z
CHEMBL13817 1958 33 None - 1 Human 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cellsAbility to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cells
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020424z
57422690 113426 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 615 8 2 10 3.8 Cc1ccn(-c2ccc(Cl)c(C(=O)NC(=O)Nc3nc4ccc(S(=O)(=O)CCCN5CCN(C)CC5)cc4s3)c2)n1 10.1021/jm500610n
CHEMBL3319227 113426 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 615 8 2 10 3.8 Cc1ccn(-c2ccc(Cl)c(C(=O)NC(=O)Nc3nc4ccc(S(=O)(=O)CCCN5CCN(C)CC5)cc4s3)c2)n1 10.1021/jm500610n
118709503 113446 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 588 7 2 9 3.8 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc5c(ccn5C)cc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319399 113446 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 588 7 2 9 3.8 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc5c(ccn5C)cc4Cl)sc3c2)CC1 10.1021/jm500610n
66788278 125166 0 None - 1 Human 9.2 pIC50 = 9.2 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 nan
CHEMBL3645254 125166 0 None - 1 Human 9.2 pIC50 = 9.2 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 nan
16114292 96905 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm701292s
CHEMBL266063 96905 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm701292s
44436850 91520 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 564 11 4 6 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL240509 91520 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 564 11 4 6 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
57422793 113443 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 631 9 2 11 3.5 COc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1021/jm500610n
CHEMBL3319396 113443 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 631 9 2 11 3.5 COc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1021/jm500610n
178024 1958 33 None - 1 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(01)00324-9
5867 1958 33 None - 1 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(01)00324-9
CHEMBL13817 1958 33 None - 1 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(01)00324-9
57422688 113424 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 601 8 2 10 3.5 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319225 113424 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 601 8 2 10 3.5 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
57785733 113423 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 612 8 2 9 4.4 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-c5ccccn5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319224 113423 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 612 8 2 9 4.4 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-c5ccccn5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
16113245 121308 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581030 121308 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2014.11.031
44445600 154764 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 542 10 2 6 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL400175 154764 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 542 10 2 6 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL437713 213708 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Ability to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) expressed in COS-7 cellsAbility to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) expressed in COS-7 cells
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C(C)C 10.1021/jm020424z
178024 1958 33 None - 1 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020985q
5867 1958 33 None - 1 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020985q
CHEMBL13817 1958 33 None - 1 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020985q
CHEMBL412799 213002 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(N)=O)C(C)C 10.1021/jm0001727
57422817 113422 18 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 620 8 2 10 3.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319223 113422 18 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 620 8 2 10 3.2 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
11476589 75959 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(CNc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205451 75959 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 456 9 3 8 4.5 Nc1nc(N)c(-c2ccc(CNc3ccc([N+](=O)[O-])cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL526723 215674 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/jm0001727
44436857 145631 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 594 12 4 7 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL391588 145631 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 594 12 4 7 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
90666039 109295 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 528 8 0 9 4.2 CCOc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218912 109295 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 528 8 0 9 4.2 CCOc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
118709505 113454 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 561 5 2 8 4.4 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319406 113454 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 561 5 2 8 4.4 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL2310887 209469 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCC(CCC)C(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C(C)C 10.1021/jm0001727
122180026 121561 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 566 7 2 7 4.4 CC(=O)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586032 121561 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 566 7 2 7 4.4 CC(=O)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
122182043 121972 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 580 7 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593632 121972 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 580 7 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL2310890 209471 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None C/C=C/C=C/C=C/C(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C(C)C 10.1021/jm0001727
44409536 75480 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 579 9 3 8 5.2 Nc1nc(N)c(-c2ccc(NCc3cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL204325 75480 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 579 9 3 8 5.2 Nc1nc(N)c(-c2ccc(NCc3cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
44445595 94374 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 572 11 2 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL250974 94374 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 572 11 2 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
90665850 109250 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 491 7 0 7 4.6 COCCN1CCC[C@@H](Cn2c(-c3ccccc3C)nc3cn(-c4ccc(Cl)cc4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218650 109250 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 491 7 0 7 4.6 COCCN1CCC[C@@H](Cn2c(-c3ccccc3C)nc3cn(-c4ccc(Cl)cc4)nc3c2=O)C1 10.1039/C2MD20340E
90665851 109251 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 459 5 0 6 4.8 Cc1ccccc1-c1nc2cn(-c3ccc(F)cc3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218651 109251 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 459 5 0 6 4.8 Cc1ccccc1-c1nc2cn(-c3ccc(F)cc3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
11134880 99403 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 500 10 6 4 2.1 O=CN[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCNCC1 10.1021/jm020985q
CHEMBL282891 99403 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 500 10 6 4 2.1 O=CN[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCNCC1 10.1021/jm020985q
5866 3597 4 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 10.1021/jm040103i
9804743 3597 4 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 10.1021/jm040103i
CHEMBL360227 3597 4 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 10.1021/jm040103i
11712151 75964 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 453 9 3 7 4.8 CC(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL205470 75964 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 453 9 3 7 4.8 CC(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
56942098 125167 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 nan
CHEMBL3645255 125167 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 nan
25261382 113414 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 535 7 2 8 3.3 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319215 113414 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 535 7 2 8 3.3 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
57422789 113428 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 629 8 2 10 4.1 Cc1cc(C)n(-c2ccc(Cl)c(C(=O)NC(=O)Nc3nc4ccc(S(=O)(=O)CCCN5CCN(C)CC5)cc4s3)c2)n1 10.1021/jm500610n
CHEMBL3319229 113428 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 629 8 2 10 4.1 Cc1cc(C)n(-c2ccc(Cl)c(C(=O)NC(=O)Nc3nc4ccc(S(=O)(=O)CCCN5CCN(C)CC5)cc4s3)c2)n1 10.1021/jm500610n
56942244 125171 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 nan
CHEMBL3645259 125171 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 nan
90665846 109246 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 491 5 0 5 6.9 Cc1ccccc1-c1nc2cc(-c3ccc(Cl)cc3)sc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218646 109246 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 491 5 0 5 6.9 Cc1ccccc1-c1nc2cc(-c3ccc(Cl)cc3)sc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
11339816 75978 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 446 8 3 7 4.7 Nc1nc(N)c(-c2ccc(NCc3ccnc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205521 75978 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 446 8 3 7 4.7 Nc1nc(N)c(-c2ccc(NCc3ccnc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
44409756 76738 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 492 8 4 8 4.1 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccc(F)cc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206820 76738 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 492 8 4 8 4.1 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccc(F)cc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
90666012 109268 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 475 5 0 6 5.3 Cc1ccccc1-c1nc2cn(-c3cccc(Cl)c3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218885 109268 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 475 5 0 6 5.3 Cc1ccccc1-c1nc2cn(-c3cccc(Cl)c3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
90666031 109287 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 498 7 0 8 4.5 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218904 109287 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 498 7 0 8 4.5 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
44390840 123530 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2cccc(Cl)c2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL361804 123530 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2cccc(Cl)c2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
90666017 109273 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 472 6 0 8 4.1 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218890 109273 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 472 6 0 8 4.1 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
90666027 109283 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 502 8 0 9 3.7 COC[C@H](C)N1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218900 109283 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 502 8 0 9 3.7 COC[C@H](C)N1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
44445594 154618 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 611 11 3 7 6.0 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL399447 154618 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 611 11 3 7 6.0 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
90666013 109269 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 471 6 0 7 4.7 COc1cccc(-n2cc3nc(-c4ccccc4C)n(CC4CCCN(C(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218886 109269 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 471 6 0 7 4.7 COc1cccc(-n2cc3nc(-c4ccccc4C)n(CC4CCCN(C(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
44445599 94155 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 581 10 3 6 6.0 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL249639 94155 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 581 10 3 6 6.0 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
44446187 94592 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252255 94592 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
178024 1958 33 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
5867 1958 33 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
CHEMBL13817 1958 33 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
23648244 91985 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
CHEMBL241775 91985 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
44409776 77114 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 7 3 7 3.5 CC(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL207754 77114 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 7 3 7 3.5 CC(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122178616 121326 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc3ccccc3cn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581048 121326 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc3ccccc3cn2)cc1 10.1016/j.bmcl.2014.11.031
16113471 84692 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 623 10 4 5 6.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(Br)cc1 10.1021/jm070024h
CHEMBL222789 84692 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 623 10 4 5 6.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(Br)cc1 10.1021/jm070024h
156021766 178103 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648355 178103 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145959787 162261 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 162261 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145953855 162491 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4167669 162491 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
16113585 137210 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 591 11 4 7 5.0 COc1ccc(Cn2c(Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
CHEMBL375161 137210 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 591 11 4 7 5.0 COc1ccc(Cn2c(Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
145958774 162242 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163811 162242 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
156016073 177631 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@@H](C)C1 10.1016/j.bmcl.2020.126953
CHEMBL4641503 177631 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@@H](C)C1 10.1016/j.bmcl.2020.126953
162646061 179507 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of GHSR-1A (unknown origin)Inhibition of GHSR-1A (unknown origin)
ChEMBL 729 18 11 12 -5.4 C[C@@H](O)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CN)NC(=O)[C@H](CO)NC(=O)CN)C(N)=O 10.1039/d0md00210k
CHEMBL4741413 179507 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of GHSR-1A (unknown origin)Inhibition of GHSR-1A (unknown origin)
ChEMBL 729 18 11 12 -5.4 C[C@@H](O)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CN)NC(=O)[C@H](CO)NC(=O)CN)C(N)=O 10.1039/d0md00210k
70692600 75845 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 447 7 0 7 2.8 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048813 75845 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 447 7 0 7 2.8 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2310886 209468 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCNC(=O)CCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C(C)C 10.1021/jm0001727
156021766 178103 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4648355 178103 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44445601 94156 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 498 8 2 5 5.4 O=C(N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1-c1ccccc1)c1ccccn1 10.1021/jm701292s
CHEMBL249640 94156 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 498 8 2 5 5.4 O=C(N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1-c1ccccc1)c1ccccn1 10.1021/jm701292s
44390901 64049 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 465 8 2 5 2.7 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc(OC)cc2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL180755 64049 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 465 8 2 5 2.7 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc(OC)cc2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
145959787 162261 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 162261 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
70694648 75843 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 462 7 0 7 3.6 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-c4nnc(C)o4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048811 75843 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 462 7 0 7 3.6 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-c4nnc(C)o4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
44445591 154617 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 591 11 4 7 5.0 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)C(C)(C)N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL399446 154617 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 591 11 4 7 5.0 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)C(C)(C)N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
16113468 141775 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
CHEMBL386218 141775 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
16113468 141775 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL386218 141775 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
46882103 5922 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 432 12 4 4 4.1 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCCN)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079872 5922 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 432 12 4 4 4.1 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCCN)cc2)cc1 10.1016/j.bmcl.2009.08.076
72190450 92246 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426679 92246 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
11441978 130429 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 437 8 2 4 4.8 CCN(CC)c1ccc(NC(=O)C2(NC(=O)OCC(C)C)CCc3ccccc3C2)cc1 10.1021/jm0491750
CHEMBL368034 130429 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 437 8 2 4 4.8 CCN(CC)c1ccc(NC(=O)C2(NC(=O)OCC(C)C)CCc3ccccc3C2)cc1 10.1021/jm0491750
CHEMBL2310894 209474 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](COC(=O)c1ccccc1)NC(=O)[C@H](CO)NC(=O)CN)C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O 10.1021/jm0001727
122180017 121552 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 525 9 2 8 4.5 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586023 121552 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 525 9 2 8 4.5 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
44445592 94154 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)C(C)(C)N)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL249638 94154 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)C(C)(C)N)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
16113577 84907 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 573 12 4 5 5.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
CHEMBL223725 84907 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 573 12 4 5 5.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
16113902 137651 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL375859 137651 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
90666041 109297 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 542 8 0 9 4.6 Cc1ncccc1-c1nc2cn(-c3cccc(OC(C)C)c3)nc2c(=O)n1C[C@H]1CCCN(C[C@H]2CCCO2)C1 10.1039/C2MD20340E
CHEMBL3218914 109297 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 542 8 0 9 4.6 Cc1ncccc1-c1nc2cn(-c3cccc(OC(C)C)c3)nc2c(=O)n1C[C@H]1CCCN(C[C@H]2CCCO2)C1 10.1039/C2MD20340E
16113902 137651 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL375859 137651 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
15945877 146914 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCCN2)cc1 10.1021/jm0704550
CHEMBL392593 146914 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCCN2)cc1 10.1021/jm0704550
11337482 76611 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
CHEMBL206399 76611 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
44409775 75996 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 8 3 7 3.7 CCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205605 75996 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 8 3 7 3.7 CCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122182190 121983 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Antagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA methodAntagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA method
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
CHEMBL3593815 121983 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Antagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA methodAntagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA method
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
44445620 154654 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 571 11 2 6 6.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccc2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL399651 154654 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 571 11 2 6 6.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccc2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
11676995 66132 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 461 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCOC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL184258 66132 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 461 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCOC)cc1 10.1016/j.bmcl.2004.06.060
16203930 84306 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 552 11 3 7 4.6 COc1cc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc(OC)c1 10.1021/jm070024h
CHEMBL221674 84306 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 552 11 3 7 4.6 COc1cc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc(OC)c1 10.1021/jm070024h
11537683 75498 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 354 5 3 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccnc(Cl)c2)cc1 10.1021/jm0510934
CHEMBL204352 75498 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 354 5 3 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccnc(Cl)c2)cc1 10.1021/jm0510934
122180020 121555 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586026 121555 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
44338247 7895 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 549 11 1 6 4.8 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=O)N1CCCN1CCCC1 10.1016/j.bmcl.2003.11.012
CHEMBL109035 7895 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 549 11 1 6 4.8 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=O)N1CCCN1CCCC1 10.1016/j.bmcl.2003.11.012
44445622 154655 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 625 11 4 7 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccc2N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL399653 154655 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 625 11 4 7 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccc2N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
59446139 81572 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 849 21 10 8 2.2 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163449 81572 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 849 21 10 8 2.2 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44436812 91735 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 11 4 6 3.9 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](C)N)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL241033 91735 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 11 4 6 3.9 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](C)N)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
11731384 162696 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 557 10 7 5 2.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCCCN1 10.1021/jm020985q
CHEMBL417092 162696 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 557 10 7 5 2.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCCCN1 10.1021/jm020985q
44390888 64386 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 435 7 2 4 2.7 CCN(CC)CCN1C(=O)C(O)(c2ccccc2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL181312 64386 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 435 7 2 4 2.7 CCN(CC)CCN1C(=O)C(O)(c2ccccc2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
60195112 81577 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 875 21 10 8 2.6 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163466 81577 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 875 21 10 8 2.6 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2370788 209898 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL None None None Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm020985q
16113904 137011 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 12 3 6 5.1 COc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL374655 137011 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 12 3 6 5.1 COc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
90665852 109252 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 466 5 0 7 4.6 Cc1ccccc1-c1nc2cn(-c3ccc(C#N)cc3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218652 109252 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 466 5 0 7 4.6 Cc1ccccc1-c1nc2cn(-c3ccc(C#N)cc3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
90666032 109288 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 512 7 0 8 4.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218905 109288 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 512 7 0 8 4.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
16113904 137011 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 550 12 3 6 5.1 COc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL374655 137011 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 550 12 3 6 5.1 COc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL500703 214097 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCNC(=N)N)C(N)=O 10.1074/jbc.m609796200
10415364 126741 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against rat Growth hormone secretagogue receptorInhibitory concentration against rat Growth hormone secretagogue receptor
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL365294 126741 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against rat Growth hormone secretagogue receptorInhibitory concentration against rat Growth hormone secretagogue receptor
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
53390181 92242 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN(C2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426675 92242 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN(C2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
145957075 162255 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164040 162255 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
145956026 162638 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4169979 162638 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145956061 162669 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4170481 162669 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
145951150 162752 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4171914 162752 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
11328064 160288 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 437 6 2 4 4.9 CCN(CC)c1ccc(NC(=O)C2(NC(=O)OC(C)(C)C)CCc3ccccc3C2)cc1 10.1021/jm0491750
CHEMBL411055 160288 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 437 6 2 4 4.9 CCN(CC)c1ccc(NC(=O)C2(NC(=O)OC(C)(C)C)CCc3ccccc3C2)cc1 10.1021/jm0491750
44445607 166706 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 572 11 2 7 5.4 COc1ccc(-n2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL428314 166706 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 572 11 2 7 5.4 COc1ccc(-n2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
16113581 85108 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1cccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL224921 85108 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1cccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
90666022 109278 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 528 7 0 9 4.2 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218895 109278 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 528 7 0 9 4.2 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
90666028 109284 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 511 7 0 10 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(Cc5cnco5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218901 109284 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 511 7 0 10 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(Cc5cnco5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
70682036 75849 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 446 7 1 4 4.3 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4n[nH]c5ccccc45)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048817 75849 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 446 7 1 4 4.3 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4n[nH]c5ccccc45)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
16113796 84652 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL222518 84652 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
57422697 113434 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 409 3 2 6 3.3 CS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319276 113434 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 409 3 2 6 3.3 CS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL499371 214072 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCC(N)=O)C(N)=O 10.1074/jbc.m609796200
59446101 81587 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 915 23 11 9 2.1 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163477 81587 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 915 23 11 9 2.1 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
59446101 81587 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 915 23 11 9 2.1 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163477 81587 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 915 23 11 9 2.1 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44389262 122006 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 479 6 2 4 6.1 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccccc1 10.1016/j.bmcl.2004.11.075
CHEMBL359506 122006 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 479 6 2 4 6.1 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccccc1 10.1016/j.bmcl.2004.11.075
16113796 84652 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL222518 84652 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
11576960 67085 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 500 8 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL187427 67085 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 500 8 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
11124146 99125 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 518 10 6 5 2.8 CCOC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL281173 99125 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 518 10 6 5 2.8 CCOC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
122178600 121310 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581033 121310 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2)cc1 10.1016/j.bmcl.2014.11.031
44409679 75479 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 466 8 4 8 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204322 75479 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 466 8 4 8 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
9745 2437 20 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
9804938 2437 20 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
CHEMBL278623 2437 20 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
DB13074 2437 20 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
16113579 84908 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 595 10 4 5 6.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1cccc2ccccc12 10.1021/jm070024h
CHEMBL223726 84908 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 595 10 4 5 6.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1cccc2ccccc12 10.1021/jm070024h
CHEMBL3578015 211743 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
145954311 162462 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4167267 162462 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL3578015 211743 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
11373823 78474 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 431 7 3 7 4.3 Nc1nc(N)c(-c2ccc(NC(=O)c3ccsc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL211188 78474 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 431 7 3 7 4.3 Nc1nc(N)c(-c2ccc(NC(=O)c3ccsc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
145954311 162462 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4167267 162462 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
44301389 11243 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1179118 11243 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL61292 11243 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
46882236 5740 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 8 4 4 4.1 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078608 5740 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 8 4 4 4.1 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
16114514 79129 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCCNC1 10.1021/jm0704550
CHEMBL2113322 79129 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCCNC1 10.1021/jm0704550
11523411 75526 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 363 6 4 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)O)cc2)cc1 10.1021/jm0510934
CHEMBL204511 75526 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 363 6 4 6 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)O)cc2)cc1 10.1021/jm0510934
57422730 113411 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 508 9 2 7 4.4 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319212 113411 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 508 9 2 7 4.4 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
46882763 5596 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [35S]MK0677 from human GHS-R1aDisplacement of [35S]MK0677 from human GHS-R1a
ChEMBL 612 17 6 7 5.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1077617 5596 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [35S]MK0677 from human GHS-R1aDisplacement of [35S]MK0677 from human GHS-R1a
ChEMBL 612 17 6 7 5.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NC[C@H](O)COc3ccc(O)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
44576247 214199 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
CHEMBL506986 214199 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1074/jbc.m609796200
145951150 162752 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4171914 162752 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21 10.1021/acs.jmedchem.8b00322
CHEMBL433540 213619 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Ability to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) expressed in COS-7 cellsAbility to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) expressed in COS-7 cells
ChEMBL None None None C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm020424z
1744826 62968 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1021/jm0491750
CHEMBL178668 62968 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1021/jm0491750
1744826 62968 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Binding affinity to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL178668 62968 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Binding affinity to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.06.060
122178603 121313 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 590 11 2 6 6.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(Cl)nc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581036 121313 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 590 11 2 6 6.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(Cl)nc2)cc1 10.1016/j.bmcl.2014.11.031
16114009 137169 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 556 10 3 5 5.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1cccc2ccccc12 10.1021/jm070024h
CHEMBL374921 137169 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 556 10 3 5 5.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1cccc2ccccc12 10.1021/jm070024h
23648246 161764 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 560 11 3 5 5.6 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
CHEMBL414132 161764 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 560 11 3 5 5.6 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
11655578 170009 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 462 8 3 7 5.2 Nc1nc(N)c(-c2ccc(NCc3cnc4ccccc4c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL444277 170009 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 462 8 3 7 5.2 Nc1nc(N)c(-c2ccc(NCc3cnc4ccccc4c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
1744826 62968 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178668 62968 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 417 6 1 4 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
156021336 178143 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 467 5 1 6 5.2 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccccc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4649089 178143 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 467 5 1 6 5.2 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccccc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
44446190 94527 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL251855 94527 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
44389167 123832 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 425 7 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL362612 123832 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 425 7 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44338240 109112 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 569 11 1 7 5.2 O=C1[C@H](CCc2ccccc2)N(Cc2cc(-c3ccccc3-c3nn[nH]n3)cs2)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
CHEMBL321403 109112 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 569 11 1 7 5.2 O=C1[C@H](CCc2ccccc2)N(Cc2cc(-c3ccccc3-c3nn[nH]n3)cs2)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
11539587 67047 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 445 8 1 4 6.7 CCCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL187271 67047 1 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 445 8 1 4 6.7 CCCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
11503585 65174 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 461 9 2 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCCO)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL182542 65174 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 461 9 2 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCCO)cc1 10.1016/j.bmcl.2004.06.060
23656300 148742 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 592 12 3 7 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2)c(OC)c1 10.1021/jm0704550
CHEMBL394054 148742 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 592 12 3 7 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2)c(OC)c1 10.1021/jm0704550
59446107 81590 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163480 81590 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
59446107 81590 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163480 81590 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(-c2ccccc2)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44436807 148287 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 547 11 3 7 4.6 COc1ccc(Cn2c(CCC3C=Nc4ccccc43)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/jm0704550
CHEMBL393692 148287 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 547 11 3 7 4.6 COc1ccc(Cn2c(CCC3C=Nc4ccccc43)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/jm0704550
46882237 5748 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 466 9 4 4 4.1 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NCCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078677 5748 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 466 9 4 4 4.1 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NCCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
44395002 66156 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 534 9 1 5 5.6 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL184368 66156 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 534 9 1 5 5.6 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)CC1 10.1016/j.bmcl.2004.06.060
44445627 154916 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 543 10 2 7 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL401084 154916 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 543 10 2 7 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
16113906 137198 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 612 12 5 5 6.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
CHEMBL375102 137198 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 612 12 5 5 6.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
70692601 75846 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 481 7 0 7 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048814 75846 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 481 7 0 7 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
145957075 162255 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164040 162255 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
145956026 162638 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4169979 162638 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 418 6 2 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)N(C)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
145956061 162669 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4170481 162669 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 3 4 2.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CN(C)CCO3)cc2c1 10.1021/acs.jmedchem.8b00322
46882271 5777 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 466 8 4 4 5.0 CCc1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078899 5777 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 466 8 4 4 5.0 CCc1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
156018364 177889 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645148 177889 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44445624 154882 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 631 11 4 7 5.8 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)[C@H]2CCCC[C@H]2N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL400879 154882 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 631 11 4 7 5.8 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)[C@H]2CCCC[C@H]2N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
16203238 137084 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 531 9 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1 10.1021/jm070024h
CHEMBL374757 137084 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 531 9 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1 10.1021/jm070024h
16113694 137168 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 609 11 4 5 6.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1cccc2ccccc12 10.1021/jm070024h
CHEMBL374920 137168 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 609 11 4 5 6.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1cccc2ccccc12 10.1021/jm070024h
16114181 141915 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 520 10 3 5 5.0 Cc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL387109 141915 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 520 10 3 5 5.0 Cc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
44446137 155393 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL403682 155393 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
122180017 121552 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 525 9 2 8 4.5 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586023 121552 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 525 9 2 8 4.5 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
44379072 12766 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 492 8 2 5 4.2 NCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1188124 12766 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 492 8 2 5 4.2 NCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL535353 12766 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 492 8 2 5 4.2 NCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
16113905 84668 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 589 12 4 6 5.6 COc1ccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL222622 84668 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 589 12 4 6 5.6 COc1ccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
11626181 124355 2 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 431 7 1 4 6.3 CCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL363896 124355 2 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 431 7 1 4 6.3 CCc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccc(N(CC)CC)cc1 10.1016/j.bmcl.2004.06.060
42624369 188839 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1713 58 25 24 -9.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
44582535 188839 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1713 58 25 24 -9.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
91935102 188839 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1713 58 25 24 -9.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
CHEMBL506930 188839 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1713 58 25 24 -9.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
16113691 136694 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
CHEMBL374073 136694 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
90666023 109279 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218896 109279 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
16113691 136694 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm0704550
CHEMBL374073 136694 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm0704550
57422696 113451 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 558 5 2 9 4.0 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319403 113451 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 558 5 2 9 4.0 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(-n5cccn5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
156012849 177274 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4636571 177274 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44390860 63614 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CC)CCN1C(=O)[C@@](O)(c2cccc(Cl)c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL180096 63614 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CC)CCN1C(=O)[C@@](O)(c2cccc(Cl)c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
73347725 92241 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 476 6 0 5 4.5 COc1ccc(CC(=O)N2CCC3(CC2)CN(Cc2ccc(-c4ncccn4)cc2Cl)C3)cc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426674 92241 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 476 6 0 5 4.5 COc1ccc(CC(=O)N2CCC3(CC2)CN(Cc2ccc(-c4ncccn4)cc2Cl)C3)cc1 10.1016/j.bmcl.2013.07.044
156012849 177274 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4636571 177274 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnc(C)c4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156015928 177557 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4640615 177557 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156018364 177889 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645148 177889 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 498 8 3 6 1.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145949595 162700 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4171040 162700 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
1100 1595 45 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None None 10.1021/jm300557t
6918297 1595 45 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None None 10.1021/jm300557t
CHEMBL108335 1595 45 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None None 10.1021/jm300557t
11539588 66883 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 445 7 1 4 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C(C)C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL186540 66883 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 445 7 1 4 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C(C)C)cc1 10.1016/j.bmcl.2004.06.060
122180015 121550 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 523 9 2 8 5.3 CCCn1cc(-c2cnc(NCc3ccc4occc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586021 121550 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 523 9 2 8 5.3 CCCn1cc(-c2cnc(NCc3ccc4occc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
122178615 121278 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2nccc3ccccc23)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3580668 121278 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 606 11 2 6 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2nccc3ccccc23)cc1 10.1016/j.bmcl.2014.11.031
16113798 84304 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 598 11 5 5 5.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
CHEMBL221662 84304 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 598 11 5 5 5.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
16113797 138112 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 637 11 4 5 6.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1ccc(Br)cc1 10.1021/jm070024h
CHEMBL376735 138112 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 637 11 4 5 6.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1ccc(Br)cc1 10.1021/jm070024h
16113903 168353 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1cc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc(OC)c1 10.1021/jm070024h
CHEMBL434573 168353 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1cc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc(OC)c1 10.1021/jm070024h
44338241 6509 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 569 11 1 7 5.2 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)s2)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
CHEMBL108287 6509 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 569 11 1 7 5.2 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)s2)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
44410012 138374 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 439 9 3 7 4.1 CCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL377305 138374 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 439 9 3 7 4.1 CCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
16113122 148144 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 538 12 3 7 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)c(OC)c1 10.1021/jm0704550
CHEMBL393565 148144 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 538 12 3 7 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)c(OC)c1 10.1021/jm0704550
11556937 81593 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163484 81593 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
11556937 81593 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163484 81593 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
9956908 13064 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 482 12 2 5 4.5 NCCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1190326 13064 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 482 12 2 5 4.5 NCCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL540604 13064 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 482 12 2 5 4.5 NCCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
11329138 64430 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 481 9 1 5 5.1 CCN(CC)c1ccc(NC(=O)C2(N(C)C(=O)OCC(C)C)CCc3cccc(OC)c3C2)cc1 10.1021/jm0491750
CHEMBL181350 64430 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 481 9 1 5 5.1 CCN(CC)c1ccc(NC(=O)C2(N(C)C(=O)OCC(C)C)CCc3cccc(OC)c3C2)cc1 10.1021/jm0491750
90665848 109248 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 507 7 0 6 6.1 COCCN1CCC[C@@H](Cn2c(-c3ccccc3C)nc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218648 109248 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 507 7 0 6 6.1 COCCN1CCC[C@@H](Cn2c(-c3ccccc3C)nc3cc(-c4ccc(Cl)cc4)sc3c2=O)C1 10.1039/C2MD20340E
23648245 91986 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
CHEMBL241776 91986 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1 10.1021/jm0704550
145949595 162700 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4171040 162700 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
11846625 77855 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 498 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(-c1ccccc1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
CHEMBL209394 77855 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 498 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(-c1ccccc1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
44409683 76230 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 480 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205848 76230 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 480 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCC3CCCC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
46882305 5796 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 494 7 4 4 5.7 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)Nc3ccc(C(C)(C)C)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079091 5796 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 494 7 4 4 5.7 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)Nc3ccc(C(C)(C)C)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
11124146 99125 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 518 10 6 5 2.8 CCOC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL281173 99125 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 518 10 6 5 2.8 CCOC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
56942855 125173 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 601 10 2 6 7.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2ccc3ccccc3c2)NC(=O)OC(C)(C)C)cc1 nan
CHEMBL3645261 125173 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 601 10 2 6 7.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2ccc3ccccc3c2)NC(=O)OC(C)(C)C)cc1 nan
11016748 98322 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 517 10 7 4 2.4 CCNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL275141 98322 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 517 10 7 4 2.4 CCNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
44445602 94157 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 537 8 3 5 5.9 O=C(N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1)c1ccccn1 10.1021/jm701292s
CHEMBL249659 94157 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 537 8 3 5 5.9 O=C(N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1)c1ccccn1 10.1021/jm701292s
11256439 75350 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 344 5 3 6 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C#N)cc2)cc1 10.1021/jm0510934
CHEMBL203843 75350 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 344 5 3 6 3.4 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C#N)cc2)cc1 10.1021/jm0510934
44390881 66073 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 465 8 2 5 2.7 CCN(CC)CCN1C(=O)[C@@](O)(c2ccccc2OC)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL183916 66073 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 465 8 2 5 2.7 CCN(CC)CCN1C(=O)[C@@](O)(c2ccccc2OC)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
44338151 109722 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 581 11 1 6 5.3 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2F)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
CHEMBL323026 109722 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 581 11 1 6 5.3 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2F)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
46882238 5751 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 7 4 4 4.7 Cc1ccccc1NC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078699 5751 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 7 4 4 4.7 Cc1ccccc1NC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
59446133 175010 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)N(Cc1ccccc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4567432 175010 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)N(Cc1ccccc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
60195284 81581 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)N(Cc1ccccc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163471 81581 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)N(Cc1ccccc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44394930 66302 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2cccc3c2OCO3)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL185028 66302 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2cccc3c2OCO3)cc1 10.1016/j.bmcl.2004.06.060
11016748 98322 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 517 10 7 4 2.4 CCNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL275141 98322 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 517 10 7 4 2.4 CCNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
59446115 174286 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)N(Cc1ccc(-c2ccccc2)cc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4550305 174286 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)N(Cc1ccc(-c2ccccc2)cc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
60195379 81585 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)N(Cc1ccc(-c2ccccc2)cc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163475 81585 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 910 22 10 9 2.6 C[C@H](NC(=O)N(Cc1ccc(-c2ccccc2)cc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
46882155 5676 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 404 8 4 4 3.3 CCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078114 5676 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 404 8 4 4 3.3 CCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
11145720 67310 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 516 11 6 4 2.9 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)NC 10.1021/jm020985q
CHEMBL18853 67310 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 516 11 6 4 2.9 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)NC 10.1021/jm020985q
11846628 77683 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 431 7 2 6 4.2 CN(C(=O)C1CCCC1)c1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
CHEMBL208930 77683 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 431 7 2 6 4.2 CN(C(=O)C1CCCC1)c1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
156015928 177557 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4640615 177557 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 512 8 3 6 1.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
16114012 168375 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 510 9 3 5 4.7 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1ccc(F)cc1 10.1021/jm070024h
CHEMBL434738 168375 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 510 9 3 5 4.7 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1ccc(F)cc1 10.1021/jm070024h
122180018 121553 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 527 9 2 9 4.3 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586024 121553 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 527 9 2 9 4.3 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
16113582 136614 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 455 7 4 5 3.5 Cn1c(Cc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL373995 136614 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 455 7 4 5 3.5 Cn1c(Cc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
46882807 5732 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 404 10 4 4 3.6 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CN)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078533 5732 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 404 10 4 4 3.6 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CN)cc2)cc1 10.1016/j.bmcl.2009.08.076
16114184 150467 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 564 11 4 7 3.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@@H](O)CN2)cc1 10.1021/jm0704550
CHEMBL395441 150467 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 564 11 4 7 3.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2C[C@@H](O)CN2)cc1 10.1021/jm0704550
44446188 155367 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL403542 155367 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
44436817 166745 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 600 13 4 6 5.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](N)Cc3ccccc3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL428383 166745 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 600 13 4 6 5.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](N)Cc3ccccc3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44445618 161874 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 570 12 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)CCc2cccnc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL415134 161874 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 570 12 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)CCc2cccnc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
44436887 90930 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 563 11 5 6 3.7 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL239464 90930 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 563 11 5 6 3.7 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
10907396 99122 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 515 10 7 5 1.2 NC1(C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2c[nH]c3ccccc23)NC=O)CCNCC1 10.1021/jm020985q
CHEMBL281147 99122 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 515 10 7 5 1.2 NC1(C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2c[nH]c3ccccc23)NC=O)CCNCC1 10.1021/jm020985q
11649239 66310 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 514 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL185057 66310 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 514 9 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
1100 1595 45 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL None None None None 10.1021/jm020985q
6918297 1595 45 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL None None None None 10.1021/jm020985q
CHEMBL108335 1595 45 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL None None None None 10.1021/jm020985q
16113580 137854 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm701292s
CHEMBL376258 137854 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm701292s
16113580 137854 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL376258 137854 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1cccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
44436883 146128 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 604 11 6 7 3.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2c[nH]c3ccccc23)cc1 10.1021/jm0704550
CHEMBL391980 146128 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 604 11 6 7 3.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2c[nH]c3ccccc23)cc1 10.1021/jm0704550
44436889 153033 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 563 11 3 5 6.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCCCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL397594 153033 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 563 11 3 5 6.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCCCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
11452801 139273 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 417 7 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)C3CCCC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL379191 139273 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 417 7 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)C3CCCC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
44445625 154795 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 612 11 3 8 5.4 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL400381 154795 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 612 11 3 8 5.4 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
122180019 121554 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586025 121554 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
145957443 162065 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
CHEMBL4160928 162065 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
10864048 98360 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.6 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL275373 98360 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.6 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
44389187 63992 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3cccc(Cl)c3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL180722 63992 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3cccc(Cl)c3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44409871 75367 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 426 7 3 8 2.4 CN(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203948 75367 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 426 7 3 8 2.4 CN(C)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145959007 162233 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163623 162233 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
145956659 162031 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4160434 162031 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
145959787 162261 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 162261 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
16113248 79135 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 560 11 3 5 5.6 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
CHEMBL2113328 79135 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 560 11 3 5 5.6 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
11282247 165902 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL425048 165902 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
11282247 165902 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL425048 165902 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 445 8 3 6 5.3 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
44409802 76715 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 439 9 3 7 4.1 CCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206687 76715 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 439 9 3 7 4.1 CCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
156019457 177918 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645625 177918 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
216208 9695 33 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
CHEMBL113313 9695 33 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
90666037 109293 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 484 6 0 8 3.8 Cc1ncccc1-c1nc2cn(-c3ccccc3)nc2c(=O)n1C[C@H]1CCCN(C[C@H]2CCCO2)C1 10.1039/C2MD20340E
CHEMBL3218910 109293 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 484 6 0 8 3.8 Cc1ncccc1-c1nc2cn(-c3ccccc3)nc2c(=O)n1C[C@H]1CCCN(C[C@H]2CCCO2)C1 10.1039/C2MD20340E
23648236 79123 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 13 3 7 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NCCN)c(OC)c1 10.1021/jm0704550
CHEMBL2113317 79123 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 13 3 7 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NCCN)c(OC)c1 10.1021/jm0704550
44383343 120316 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 606 6 2 5 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3Cc4ccccc4CN3)CC2)c2ccccc21 10.1021/jm0309452
CHEMBL353007 120316 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 606 6 2 5 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)C3Cc4ccccc4CN3)CC2)c2ccccc21 10.1021/jm0309452
156014693 177168 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 530 6 2 8 2.9 CCOc1cc(Cl)c(-c2ccc(-c3nc4c(s3)CN(C(=O)CO)CC4)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4635089 177168 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 530 6 2 8 2.9 CCOc1cc(Cl)c(-c2ccc(-c3nc4c(s3)CN(C(=O)CO)CC4)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
44389151 62475 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 445 6 1 4 5.7 CCN(CC)C(=O)c1ccccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
CHEMBL178138 62475 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 445 6 1 4 5.7 CCN(CC)C(=O)c1ccccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
44409979 140534 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 7 2 7 3.4 CCc1nc(N)nc(N(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL381159 140534 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 7 2 7 3.4 CCc1nc(N)nc(N(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44395020 124006 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 507 9 1 5 6.1 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL363021 124006 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 507 9 1 5 6.1 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)CC1 10.1016/j.bmcl.2004.06.060
16114530 84711 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 539 13 4 5 5.7 CCCCCCn1c(CCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL222912 84711 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 539 13 4 5 5.7 CCCCCCn1c(CCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
59446130 81589 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 800 21 10 9 0.4 CC(C)CN(NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163479 81589 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 800 21 10 9 0.4 CC(C)CN(NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
59446130 81589 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 800 21 10 9 0.4 CC(C)CN(NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163479 81589 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 800 21 10 9 0.4 CC(C)CN(NC(=O)[C@H](C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44409761 75837 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 9 3 7 4.4 CCc1nc(N)nc(NCC(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204880 75837 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 9 3 7 4.4 CCc1nc(N)nc(NCC(C)C)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145956659 162031 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4160434 162031 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 406 4 4 3 2.4 O=C(N[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H]1CCNC1)c1cc2cc(F)ccc2[nH]1 10.1021/acs.jmedchem.8b00322
145957443 162065 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
CHEMBL4160928 162065 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
145959007 162233 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163623 162233 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 436 4 4 5 2.8 N#Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
145959787 162261 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164107 162261 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 444 4 2 4 3.4 CN1CCCCC(C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
11328920 144017 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 471 8 2 4 5.4 CCN(CC)c1ccc(NC(=O)C2(NC(=O)OCC(C)C)CCc3cccc(Cl)c3C2)cc1 10.1021/jm0491750
CHEMBL390308 144017 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 471 8 2 4 5.4 CCN(CC)c1ccc(NC(=O)C2(NC(=O)OCC(C)C)CCc3cccc(Cl)c3C2)cc1 10.1021/jm0491750
122178606 121316 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(F)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581039 121316 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(F)n2)cc1 10.1016/j.bmcl.2014.11.031
122178609 121320 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 586 12 2 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(OC)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581042 121320 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 586 12 2 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(OC)n2)cc1 10.1016/j.bmcl.2014.11.031
178024 1958 33 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
5867 1958 33 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
CHEMBL13817 1958 33 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/acs.jmedchem.8b00322
44409821 76008 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 564 10 4 8 4.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CCC(=O)NCc3cccc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205711 76008 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 564 10 4 8 4.2 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CCC(=O)NCc3cccc(Cl)c3)cc2)cc1 10.1016/j.bmcl.2006.01.012
46882307 5798 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 530 8 4 4 6.0 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NC(C)(C)c3cccc4ccccc34)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079108 5798 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 530 8 4 4 6.0 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NC(C)(C)c3cccc4ccccc34)cc2)cc1 10.1016/j.bmcl.2009.08.076
122182044 121973 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 552 9 2 6 4.9 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593633 121973 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 552 9 2 6 4.9 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
5866 3597 4 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 10.1016/j.bmcl.2005.02.042
9804743 3597 4 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 10.1016/j.bmcl.2005.02.042
CHEMBL360227 3597 4 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CCN1c2cc(cc(c2[C@](C1=O)(O)c1ccccc1Cl)C(F)(F)F)C(=O)N)CC 10.1016/j.bmcl.2005.02.042
CHEMBL500468 214092 0 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1021/jm501702q
CHEMBL500468 214092 0 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1021/jm501702q
11683469 76677 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 433 6 3 7 3.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(C)(=O)=O)c(F)c2)cc1 10.1021/jm0510934
CHEMBL206486 76677 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 433 6 3 7 3.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(C)(=O)=O)c(F)c2)cc1 10.1021/jm0510934
11454617 141294 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 488 8 3 8 4.0 CN(Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2006.01.012
CHEMBL383411 141294 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 488 8 3 8 4.0 CN(Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2006.01.012
90666029 109285 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 510 7 0 9 4.5 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(Cc5ccco5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218902 109285 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 510 7 0 9 4.5 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(Cc5ccco5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
44409672 140462 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 479 9 3 9 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccco3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL380971 140462 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 479 9 3 9 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccco3)cc2)cc1 10.1016/j.bmcl.2006.01.012
11154823 76000 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 436 8 3 7 4.5 N#Cc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL205660 76000 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 436 8 3 7 4.5 N#Cc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
11190594 75956 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 469 10 3 8 3.9 CC(C)CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205445 75956 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 469 10 3 8 3.9 CC(C)CCOCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
11583811 75958 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 479 8 3 6 5.7 Nc1nc(N)c(-c2ccc(NCc3ccc(C(F)(F)F)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205450 75958 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 479 8 3 6 5.7 Nc1nc(N)c(-c2ccc(NCc3ccc(C(F)(F)F)cc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
25260900 113450 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 593 10 2 9 4.3 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(N4CCOCC4)ccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319402 113450 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 593 10 2 9 4.3 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(N4CCOCC4)ccc3Cl)sc2c1 10.1021/jm500610n
10918326 98944 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N(C)C 10.1021/jm020985q
CHEMBL279822 98944 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N(C)C 10.1021/jm020985q
44378981 13938 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 504 10 2 5 5.5 NCCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1196773 13938 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 504 10 2 5 5.5 NCCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL558181 13938 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 504 10 2 5 5.5 NCCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
90666033 109289 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 526 7 0 8 5.3 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCCC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218906 109289 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 526 7 0 8 5.3 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCCC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
16113472 168982 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2ccccc2)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL439251 168982 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2ccccc2)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
66813470 76803 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]ghrelin from GHS receptorDisplacement of [125I]ghrelin from GHS receptor
ChEMBL 459 6 2 6 3.3 O=C(N[C@@H]1COc2cccc(-c3ccc(CO)nc3)c2C1)c1ccc(OCC(F)(F)F)nc1 10.1016/j.bmcl.2012.06.105
CHEMBL2069411 76803 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]ghrelin from GHS receptorDisplacement of [125I]ghrelin from GHS receptor
ChEMBL 459 6 2 6 3.3 O=C(N[C@@H]1COc2cccc(-c3ccc(CO)nc3)c2C1)c1ccc(OCC(F)(F)F)nc1 10.1016/j.bmcl.2012.06.105
122180022 121557 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 504 7 2 9 2.8 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2CCOCC2)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
CHEMBL3586028 121557 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 504 7 2 9 2.8 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2CCOCC2)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
70694649 75855 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 475 5 0 7 3.2 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-n3nccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
CHEMBL2048823 75855 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 475 5 0 7 3.2 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-n3nccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
10100708 12002 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 530 9 3 7 0.3 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@@H](N)CO)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL1183387 12002 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 530 9 3 7 0.3 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@@H](N)CO)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL294408 12002 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 530 9 3 7 0.3 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@@H](N)CO)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
11577349 65201 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 529 9 1 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCN(C)C2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL182655 65201 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 529 9 1 5 5.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCN(C)C2=O)cc1 10.1016/j.bmcl.2004.06.060
16114098 141586 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 534 11 3 5 5.4 Cc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL385131 141586 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 534 11 3 5 5.4 Cc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
11327400 75343 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 412 8 3 7 4.0 Nc1nc(N)c(-c2ccc(NCc3ccncc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL203782 75343 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 412 8 3 7 4.0 Nc1nc(N)c(-c2ccc(NCc3ccncc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
44409455 75939 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 487 6 3 7 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c2)cc1 10.1021/jm0510934
CHEMBL205286 75939 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 487 6 3 7 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2cc(F)c(S(=O)(=O)C(F)(F)F)c(F)c2)cc1 10.1021/jm0510934
156019457 177918 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645625 177918 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
46882306 5797 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 502 8 4 4 5.2 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NCc3cccc4ccccc34)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079107 5797 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 502 8 4 4 5.2 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)NCc3cccc4ccccc34)cc2)cc1 10.1016/j.bmcl.2009.08.076
11731384 162696 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 557 10 7 5 2.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCCCN1 10.1021/jm020985q
CHEMBL417092 162696 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 557 10 7 5 2.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCCCN1 10.1021/jm020985q
118709470 113432 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 395 3 2 5 4.6 COc1ccc2nc(NC(=O)NC(=O)c3c(Cl)cccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319274 113432 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 395 3 2 5 4.6 COc1ccc2nc(NC(=O)NC(=O)c3c(Cl)cccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL507636 214410 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@H]1CCCN1C(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1074/jbc.m609796200
156021885 178191 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 635 10 1 10 4.2 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1CCO[C@H](C)C1 10.1016/j.bmcl.2020.126953
CHEMBL4649741 178191 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 635 10 1 10 4.2 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1CCO[C@H](C)C1 10.1016/j.bmcl.2020.126953
70688404 75838 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048807 75838 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1016/j.bmcl.2012.05.024
11114279 98221 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 544 12 6 4 3.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(C)C 10.1021/jm020985q
CHEMBL274460 98221 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 544 12 6 4 3.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(C)C 10.1021/jm020985q
70688404 75838 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1016/j.bmcl.2013.07.044
CHEMBL2048807 75838 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1016/j.bmcl.2013.07.044
16113693 137991 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 589 12 4 6 5.6 COc1cccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL376471 137991 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 589 12 4 6 5.6 COc1cccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
216208 9695 33 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
CHEMBL113313 9695 33 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1021/acs.jmedchem.8b00322
11827047 99192 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 488 11 6 4 2.1 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC=O 10.1021/jm020985q
CHEMBL281578 99192 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 488 11 6 4 2.1 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC=O 10.1021/jm020985q
9745 2437 20 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
9804938 2437 20 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
CHEMBL278623 2437 20 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
DB13074 2437 20 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 10.1021/jm020985q
16113124 121309 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccncc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581032 121309 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 556 11 2 6 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccncc2)cc1 10.1016/j.bmcl.2014.11.031
44445605 154957 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 542 10 2 6 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccncc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL401260 154957 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 542 10 2 6 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccncc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
16113578 137167 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 542 9 3 5 5.7 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1cccc2ccccc12 10.1021/jm070024h
CHEMBL374919 137167 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 542 9 3 5 5.7 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1cccc2ccccc12 10.1021/jm070024h
16113584 137569 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 441 7 5 4 3.5 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2c[nH]c3ccccc23)[nH]1 10.1021/jm070024h
CHEMBL375568 137569 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 441 7 5 4 3.5 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2c[nH]c3ccccc23)[nH]1 10.1021/jm070024h
44389168 64843 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 457 4 1 4 5.8 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCC1 10.1016/j.bmcl.2004.11.075
CHEMBL182154 64843 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 457 4 1 4 5.8 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCC1 10.1016/j.bmcl.2004.11.075
11314908 141787 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 377 7 3 6 3.4 CCC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
CHEMBL386290 141787 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 377 7 3 6 3.4 CCC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
11846627 79695 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 363 6 3 6 3.0 CC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
CHEMBL211581 79695 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 363 6 3 6 3.0 CC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
10929048 68778 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 488 9 6 4 2.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL19220 68778 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 488 9 6 4 2.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
90666020 109276 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 500 7 0 9 3.5 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218893 109276 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 500 7 0 9 3.5 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
16114403 147162 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2)cc1 10.1021/jm0704550
CHEMBL392805 147162 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCCN2)cc1 10.1021/jm0704550
57422673 113439 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 474 4 2 7 4.1 CS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(-n4cccc4)ccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319282 113439 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 474 4 2 7 4.1 CS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(-n4cccc4)ccc3Cl)sc2c1 10.1021/jm500610n
70684154 75840 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 414 6 0 4 3.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccccc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048809 75840 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 414 6 0 4 3.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccccc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
122180020 121555 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586026 121555 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
16113710 79132 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCNCC1 10.1021/jm0704550
CHEMBL2113325 79132 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 571 10 4 5 5.5 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1)C1CCNCC1 10.1021/jm0704550
122178611 121322 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 572 11 3 7 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2O)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581044 121322 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 572 11 3 7 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2O)cc1 10.1016/j.bmcl.2014.11.031
122178614 121325 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 660 13 2 7 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2C(=O)c2ccccc2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581047 121325 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 660 13 2 7 6.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2C(=O)c2ccccc2)cc1 10.1016/j.bmcl.2014.11.031
16114531 84646 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 553 14 4 5 6.1 CCCCCCn1c(CCCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL222498 84646 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 553 14 4 5 6.1 CCCCCCn1c(CCCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
145974293 163000 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4175823 163000 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
46882197 5710 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 432 10 4 4 4.1 CCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078403 5710 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 432 10 4 4 4.1 CCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
44409980 76151 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 8 3 7 3.7 CCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205790 76151 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 425 8 3 7 3.7 CCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145952740 162477 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4167481 162477 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
44409868 76713 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 487 9 3 7 4.9 CCc1nc(N)nc(NCc2ccccc2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206673 76713 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 487 9 3 7 4.9 CCc1nc(N)nc(NCc2ccccc2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
156017532 177884 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645072 177884 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
11605822 124362 1 None - 0 Human 7.6 pIC50 = 7.6 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 503 9 1 6 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL363930 124362 1 None - 0 Human 7.6 pIC50 = 7.6 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 503 9 1 6 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCO2)cc1 10.1016/j.bmcl.2004.06.060
162651761 180185 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting methodDisplacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting method
ChEMBL 798 19 7 8 3.0 NCCCC[C@H](NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)C(N)=O 10.1016/j.ejmech.2016.07.078
CHEMBL4749698 180185 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting methodDisplacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting method
ChEMBL 798 19 7 8 3.0 NCCCC[C@H](NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)C(N)=O 10.1016/j.ejmech.2016.07.078
70686292 75851 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 461 5 0 8 3.0 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048819 75851 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 461 5 0 8 3.0 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
10186158 98414 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
CHEMBL275660 98414 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
122178602 121312 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2Br)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581035 121312 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2Br)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3586019 211778 6 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CCCNC(=N)N)C(N)=O 10.1016/j.bmcl.2015.04.040
122180025 121560 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 542 7 2 8 3.6 CC(=O)N1CC=C(c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)CC1 10.1016/j.bmcl.2015.04.040
CHEMBL3586031 121560 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 542 7 2 8 3.6 CC(=O)N1CC=C(c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)CC1 10.1016/j.bmcl.2015.04.040
156017532 177884 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4645072 177884 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145952740 162477 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
CHEMBL4167481 162477 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21 10.1021/acs.jmedchem.8b00322
145974293 163000 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4175823 163000 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
44436881 91559 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 540 10 4 6 4.6 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1Cc1cccs1)C1CCNCC1 10.1021/jm0704550
CHEMBL240746 91559 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 540 10 4 6 4.6 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1Cc1cccs1)C1CCNCC1 10.1021/jm0704550
122182189 121982 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593814 121982 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
122180016 121551 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 540 9 2 9 5.1 CCCn1cc(-c2cnc(NCc3ccc4ncsc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586022 121551 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 540 9 2 9 5.1 CCCn1cc(-c2cnc(NCc3ccc4ncsc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
46882199 5729 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 438 7 4 4 4.4 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)Nc3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078498 5729 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 438 7 4 4 4.4 CC(C)(N)Cc1ccc(NS(=O)(=O)c2ccc(NC(=O)Nc3ccccc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
44301462 11230 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1179075 11230 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL58758 11230 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 623 15 4 9 0.2 CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
90666042 109298 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 550 8 0 9 4.4 Cc1ncccc1-c1nc2cn(-c3cccc(OC(F)F)c3)nc2c(=O)n1C[C@H]1CCCN(C[C@H]2CCCO2)C1 10.1039/C2MD20340E
CHEMBL3218915 109298 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 550 8 0 9 4.4 Cc1ncccc1-c1nc2cn(-c3cccc(OC(F)F)c3)nc2c(=O)n1C[C@H]1CCCN(C[C@H]2CCCO2)C1 10.1039/C2MD20340E
25262771 113437 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 480 7 3 7 3.7 CC(C)NCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319280 113437 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 480 7 3 7 3.7 CC(C)NCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
42624370 188813 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1797 64 25 24 -7.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
44582537 188813 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1797 64 25 24 -7.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
91935104 188813 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1797 64 25 24 -7.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
CHEMBL506624 188813 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1797 64 25 24 -7.0 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
44445617 154652 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 556 11 2 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccncc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL399649 154652 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 556 11 2 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccncc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
11163070 65538 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 322 5 1 2 4.3 CCN(CC)c1ccc(NC(=O)C2CCc3ccccc3C2)cc1 10.1021/jm0491750
CHEMBL183123 65538 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 322 5 1 2 4.3 CCN(CC)c1ccc(NC(=O)C2CCc3ccccc3C2)cc1 10.1021/jm0491750
156012428 177286 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@H](C)C1 10.1016/j.bmcl.2020.126953
CHEMBL4636832 177286 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 649 10 1 10 4.6 CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)cc1N1C[C@H](C)O[C@H](C)C1 10.1016/j.bmcl.2020.126953
46882766 5640 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 418 11 4 4 3.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCN)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1077839 5640 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 418 11 4 4 3.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCN)cc2)cc1 10.1016/j.bmcl.2009.08.076
44436813 147282 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 11 4 5 4.5 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](C)N)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL392902 147282 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 11 4 5 4.5 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](C)N)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44410013 77024 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 10 3 7 4.5 CCCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL207268 77024 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 10 3 7 4.5 CCCCNc1nc(N)nc(CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44235473 81588 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163478 81588 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
44235473 81588 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163478 81588 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 834 21 10 9 0.9 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44409839 76229 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 412 7 4 8 2.0 CNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205847 76229 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 412 7 4 8 2.0 CNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
16114099 137199 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 559 10 4 5 5.5 Cc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL375103 137199 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 559 10 4 5 5.5 Cc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
16113372 79125 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCN2)cc1 10.1021/jm0704550
CHEMBL2113319 79125 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCN2)cc1 10.1021/jm0704550
46882273 5786 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 494 10 4 4 5.8 CCCCc1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078982 5786 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 494 10 4 4 5.8 CCCCc1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
122182044 121973 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 552 9 2 6 4.9 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593633 121973 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 552 9 2 6 4.9 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
121879 2222 24 None - 1 Human 5.6 pIC50 = 5.6 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
5868 2222 24 None - 1 Human 5.6 pIC50 = 5.6 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
CHEMBL308716 2222 24 None - 1 Human 5.6 pIC50 = 5.6 Binding
Inhibition against human growth hormone secretagogue (GHS) receptorInhibition against human growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
CHEMBL2370788 209898 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL None None None Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm020985q
145950261 162705 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4171137 162705 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
44394974 66982 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 515 9 1 5 7.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCOCC2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL186974 66982 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 515 9 1 5 7.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCOCC2)cc1 10.1016/j.bmcl.2004.06.060
44445615 161845 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 556 11 2 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2cccnc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL414929 161845 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 556 11 2 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2cccnc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
16113370 79130 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCCN2)cc1 10.1021/jm0704550
CHEMBL2113323 79130 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCCN2)cc1 10.1021/jm0704550
145953016 162563 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
CHEMBL4168863 162563 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
156012445 177311 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637284 177311 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
10186158 98414 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
CHEMBL275660 98414 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N(C)[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
11617435 75968 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 359 5 3 6 4.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2csc(Cl)c2)cc1 10.1021/jm0510934
CHEMBL205486 75968 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 359 5 3 6 4.2 CCc1nc(N)nc(N)c1-c1ccc(NCc2csc(Cl)c2)cc1 10.1021/jm0510934
70696689 75853 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 460 5 0 7 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5cccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048821 75853 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 460 5 0 7 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5cccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
70694647 75839 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 380 6 0 4 3.2 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccccc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048808 75839 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 380 6 0 4 3.2 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccccc2)C3)cc1 10.1016/j.bmcl.2012.05.024
56942242 125169 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 nan
CHEMBL3645257 125169 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 nan
122178605 121315 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581038 121315 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 574 11 2 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2014.11.031
44445611 154651 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 556 11 2 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL399648 154651 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 556 11 2 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
122182189 121982 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593814 121982 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from human ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
56942385 125172 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 nan
CHEMBL3645260 125172 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 nan
CHEMBL501261 214112 23 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)CCCNC(=N)N)C(N)=O 10.1074/jbc.m609796200
56942099 125168 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 nan
CHEMBL3645256 125168 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 nan
56942243 125170 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 nan
CHEMBL3645258 125170 0 None - 1 Human 8.5 pIC50 = 8.5 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 nan
122178608 121319 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 570 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(C)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581041 121319 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 570 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(C)n2)cc1 10.1016/j.bmcl.2014.11.031
44409673 76721 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 493 9 3 9 3.9 Cc1ccc(COCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)o1 10.1016/j.bmcl.2006.01.012
CHEMBL206741 76721 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 493 9 3 9 3.9 Cc1ccc(COCc2nc(N)nc(N)c2-c2ccc(NCc3ccc(S(C)(=O)=O)cc3)cc2)o1 10.1016/j.bmcl.2006.01.012
CHEMBL105462 208445 38 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
11690097 76643 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 411 6 2 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(N(C)Cc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
CHEMBL206446 76643 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 411 6 2 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(N(C)Cc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
57422695 113449 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 574 10 2 9 4.6 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(-n4cccn4)ccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319401 113449 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 574 10 2 9 4.6 CCN(CC)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3cc(-n4cccn4)ccc3Cl)sc2c1 10.1021/jm500610n
25124566 1861 8 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 10.1021/jm5003183
5870 1861 8 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 10.1021/jm5003183
CHEMBL3358452 1861 8 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 487 5 2 5 4.1 O=C([C@@H](c1cccnc1)N1CCN2[C@@H](C1)CCC2)NNc1cc(cc(c1)C(F)(F)F)C(F)(F)F 10.1021/jm5003183
156013219 177465 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639379 177465 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145957574 162277 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164328 162277 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
46882805 5792 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 474 13 4 4 5.1 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NCC)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079046 5792 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 474 13 4 4 5.1 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NCC)cc2)cc1 10.1016/j.bmcl.2009.08.076
53390538 92248 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 474 5 0 6 4.4 COc1ccc(CC(=O)N2CCC3(CC2)CN(C2CCc4cc(-c5nccs5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426681 92248 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 474 5 0 6 4.4 COc1ccc(CC(=O)N2CCC3(CC2)CN(C2CCc4cc(-c5nccs5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
178024 1958 33 None - 1 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(99)00584-3
5867 1958 33 None - 1 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(99)00584-3
CHEMBL13817 1958 33 None - 1 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1016/s0960-894x(99)00584-3
44445629 161876 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 559 10 2 8 4.9 COc1ccc(-n2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL415136 161876 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 559 10 2 8 4.9 COc1ccc(-n2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
16204239 136259 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
CHEMBL373393 136259 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
11508639 76506 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(Cl)cc2)cc1 10.1021/jm0510934
CHEMBL206091 76506 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(Cl)cc2)cc1 10.1021/jm0510934
216208 9695 33 None - 1 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1016/s0960-894x(99)00584-3
CHEMBL113313 9695 33 None - 1 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1016/s0960-894x(99)00584-3
11846630 138910 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 426 7 3 7 3.7 Nc1nc(N)c(-c2ccc(NC(=O)c3ccncc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL378438 138910 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 426 7 3 7 3.7 Nc1nc(N)c(-c2ccc(NC(=O)c3ccncc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
156012445 177311 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637284 177311 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cnccn4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145953016 162563 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
CHEMBL4168863 162563 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1 10.1021/acs.jmedchem.8b00322
145949755 162910 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174302 162910 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
16204241 84399 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 520 11 3 5 4.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1CCc1ccccc1 10.1021/jm070024h
CHEMBL221996 84399 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 520 11 3 5 4.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1CCc1ccccc1 10.1021/jm070024h
11221946 140821 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm0510934
CHEMBL381942 140821 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm0510934
11221946 140821 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm060461g
CHEMBL381942 140821 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 353 5 3 5 4.1 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(Cl)cc2)cc1 10.1021/jm060461g
46882104 5923 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 460 12 4 4 4.9 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079873 5923 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 460 12 4 4 4.9 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CCC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
145956415 162039 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160541 162039 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145950261 162705 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4171137 162705 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
11654867 76172 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 429 7 3 5 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(CCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205833 76172 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 429 7 3 5 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)cc3)cc2)c(CCc2ccccc2)n1 10.1021/jm0510934
10415364 126741 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL365294 126741 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
178024 1958 33 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020985q
5867 1958 33 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020985q
CHEMBL13817 1958 33 None - 1 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm020985q
16114404 154873 24 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 508 11 3 6 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL400814 154873 24 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 508 11 3 6 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1016/j.bmcl.2014.11.031
90666014 109270 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 466 5 0 7 4.6 Cc1ccccc1-c1nc2cn(-c3cccc(C#N)c3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL3218887 109270 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 466 5 0 7 4.6 Cc1ccccc1-c1nc2cn(-c3cccc(C#N)c3)nc2c(=O)n1CC1CCCN(C(C)C)C1 10.1039/C2MD20340E
44436885 146404 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 634 12 6 8 3.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2c[nH]c3ccccc23)c(OC)c1 10.1021/jm0704550
CHEMBL392191 146404 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 634 12 6 8 3.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2c[nH]c3ccccc23)c(OC)c1 10.1021/jm0704550
44436829 152454 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 11 4 6 4.3 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL397109 152454 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 11 4 6 4.3 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
16114404 154873 24 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 508 11 3 6 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/jm0704550
CHEMBL400814 154873 24 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 508 11 3 6 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/jm0704550
122182047 121976 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA methodAntagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA method
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593636 121976 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA methodAntagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA method
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
70684155 75856 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 486 5 0 6 4.1 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-c3ncccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
CHEMBL2048824 75856 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 486 5 0 6 4.1 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-c3ncccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
CHEMBL2163483 209302 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163483 209302 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44409872 75037 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 467 7 2 8 3.1 CCc1nc(N)nc(N2CCOCC2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203581 75037 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 467 7 2 8 3.1 CCc1nc(N)nc(N2CCOCC2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44445596 154619 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 558 10 2 7 5.5 COc1ccc(-n2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL399448 154619 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 558 10 2 7 5.5 COc1ccc(-n2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
16113692 137211 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 559 11 4 5 5.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
CHEMBL375162 137211 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 559 11 4 5 5.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm070024h
118709504 113452 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 572 5 2 9 4.3 Cc1ccnn1-c1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
CHEMBL3319404 113452 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 572 5 2 9 4.3 Cc1ccnn1-c1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
10907396 99122 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 515 10 7 5 1.2 NC1(C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2c[nH]c3ccccc23)NC=O)CCNCC1 10.1021/jm020985q
CHEMBL281147 99122 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 515 10 7 5 1.2 NC1(C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](Cc2c[nH]c3ccccc23)NC=O)CCNCC1 10.1021/jm020985q
11677781 125032 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 502 9 1 5 5.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN(C)C(C)=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL364430 125032 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 502 9 1 5 5.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN(C)C(C)=O)cc1 10.1016/j.bmcl.2004.06.060
44445606 154990 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 625 12 3 7 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL401467 154990 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 625 12 3 7 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
44379034 12892 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 490 9 2 5 5.1 NCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1189120 12892 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 490 9 2 5 5.1 NCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL538068 12892 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 490 9 2 5 5.1 NCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
44378986 13063 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 470 10 2 5 3.2 NCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1190325 13063 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 470 10 2 5 3.2 NCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL540603 13063 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 470 10 2 5 3.2 NCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
11697618 62569 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 427 6 1 4 5.5 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Br)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178289 62569 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 427 6 1 4 5.5 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Br)noc2C)cc1 10.1016/j.bmcl.2004.11.075
145956415 162039 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160541 162039 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
44436886 161931 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 595 12 5 8 3.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL415674 161931 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 595 12 5 8 3.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
145949755 162910 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174302 162910 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1 10.1021/acs.jmedchem.8b00322
23648242 79127 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 571 10 4 5 5.7 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1021/jm0704550
CHEMBL2113320 79127 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 571 10 4 5 5.7 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1021/jm0704550
11606121 64546 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 523 6 2 6 5.9 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.11.075
CHEMBL181584 64546 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 523 6 2 6 5.9 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.11.075
122180023 121558 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 530 7 2 8 3.8 C[C@H]1CN(c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)C[C@@H](C)O1 10.1016/j.bmcl.2015.04.040
CHEMBL3586029 121558 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 530 7 2 8 3.8 C[C@H]1CN(c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)C[C@@H](C)O1 10.1016/j.bmcl.2015.04.040
44379301 13028 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 506 9 2 7 3.7 COC(=O)C(CCCCN)NC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Cl)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1190091 13028 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 506 9 2 7 3.7 COC(=O)C(CCCCN)NC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Cl)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL540093 13028 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 506 9 2 7 3.7 COC(=O)C(CCCCN)NC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Cl)cc2c1=O 10.1016/s0960-894x(99)00584-3
44338300 167819 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 525 10 1 6 4.0 CN(C)CCCN1C(=O)[C@H](Cc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=S 10.1016/j.bmcl.2003.11.012
CHEMBL430882 167819 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 525 10 1 6 4.0 CN(C)CCCN1C(=O)[C@H](Cc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=S 10.1016/j.bmcl.2003.11.012
44338239 167874 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 511 9 1 6 4.2 CN(C)CCCN1C(=O)[C@H](c2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=S 10.1016/j.bmcl.2003.11.012
CHEMBL431245 167874 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 511 9 1 6 4.2 CN(C)CCCN1C(=O)[C@H](c2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=S 10.1016/j.bmcl.2003.11.012
44409762 75857 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 441 9 4 8 2.7 CCc1nc(N)nc(NCCO)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204884 75857 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 441 9 4 8 2.7 CCc1nc(N)nc(NCCO)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122180018 121553 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 527 9 2 9 4.3 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586024 121553 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 527 9 2 9 4.3 CCCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
122182189 121982 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Antagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA methodAntagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA method
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593814 121982 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Antagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA methodAntagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA method
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
10032659 12019 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 587 11 4 8 -0.5 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@H](CO)NC(=O)CN)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL1183505 12019 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 587 11 4 8 -0.5 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@H](CO)NC(=O)CN)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
CHEMBL301259 12019 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 587 11 4 8 -0.5 CS(=O)(=O)N1CC2(CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)[C@H](CO)NC(=O)CN)CC2)c2ccccc21 10.1016/s0960-894x(01)00324-9
60195019 81575 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 849 21 10 8 2.2 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163464 81575 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 849 21 10 8 2.2 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](C)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
156009875 177099 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633695 177099 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
11430583 80188 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 439 8 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL213704 80188 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 439 8 3 6 4.2 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
11517629 168314 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 431 6 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C)c1 10.1016/j.bmcl.2004.11.075
CHEMBL434330 168314 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 431 6 1 4 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C)c1 10.1016/j.bmcl.2004.11.075
44409975 75761 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 411 7 3 7 3.3 CCc1nc(N)nc(NC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204835 75761 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 411 7 3 7 3.3 CCc1nc(N)nc(NC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
53391301 92245 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN(C2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426678 92245 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN(C2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
90666019 109275 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 464 7 0 8 3.8 COCCN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(C4CCCCC4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218892 109275 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 464 7 0 8 3.8 COCCN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(C4CCCCC4)nc3c2=O)C1 10.1039/C2MD20340E
11669486 64584 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 445 7 1 4 6.6 CCc1cc(N(CC)CC)ccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
CHEMBL181736 64584 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 445 7 1 4 6.6 CCc1cc(N(CC)CC)ccc1NC(=O)c1c(-c2c(Cl)cccc2Cl)noc1C 10.1016/j.bmcl.2004.11.075
59446141 81591 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(CCc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163481 81591 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(CCc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
59446141 81591 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(CCc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163481 81591 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(CCc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44436917 90620 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 4 5 5.3 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL239007 90620 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 4 5 5.3 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
60165265 116172 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 453 5 1 2 6.0 CC(NC(=O)N(Cc1ccccc1Cl)C1CCN(C)CC1)c1cccc(Cl)c1Cl 10.1021/jm5003183
CHEMBL3358453 116172 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 453 5 1 2 6.0 CC(NC(=O)N(Cc1ccccc1Cl)C1CCN(C)CC1)c1cccc(Cl)c1Cl 10.1021/jm5003183
16113002 148289 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 577 12 4 7 4.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)c(OC)c1 10.1021/jm0704550
CHEMBL393693 148289 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 577 12 4 7 4.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)c(OC)c1 10.1021/jm0704550
44409678 141192 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 490 9 3 9 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3cccnc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL382853 141192 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 490 9 3 9 3.4 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3cccnc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
122178604 121314 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2N)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581037 121314 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccnc2N)cc1 10.1016/j.bmcl.2014.11.031
10929048 68778 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 488 9 6 4 2.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL19220 68778 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 488 9 6 4 2.2 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
60195018 81574 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 834 21 9 7 3.2 CCC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NN(CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163463 81574 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 834 21 9 7 3.2 CCC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NN(CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44394913 127147 1 None - 0 Human 6.4 pIC50 = 6.4 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 537 10 1 5 7.5 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccccc2OC)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL365721 127147 1 None - 0 Human 6.4 pIC50 = 6.4 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 537 10 1 5 7.5 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccccc2OC)cc1 10.1016/j.bmcl.2004.06.060
11649248 66640 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 515 9 1 5 7.2 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL185399 66640 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 515 9 1 5 7.2 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCCO2)cc1 10.1016/j.bmcl.2004.06.060
44394833 126799 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 542 9 1 5 6.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2C(=O)CCC2(C)C)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL365460 126799 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 542 9 1 5 6.7 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2C(=O)CCC2(C)C)cc1 10.1016/j.bmcl.2004.06.060
11827047 99192 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 488 11 6 4 2.1 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC=O 10.1021/jm020985q
CHEMBL281578 99192 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 488 11 6 4 2.1 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC=O 10.1021/jm020985q
42624359 193377 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1755 61 25 24 -8.1 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
44582536 193377 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1755 61 25 24 -8.1 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
91935103 193377 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1755 61 25 24 -8.1 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
CHEMBL525751 193377 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cellsDisplacement of [125I]ghrelin from human growth hormone secretagogue receptor expressed in CHO-K1 cells
ChEMBL 1755 61 25 24 -8.1 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CNC(=O)CCCCCCCCF)NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O)C(C)C 10.1021/jm8014519
156009875 177099 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633695 177099 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 499 8 3 7 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccnnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156021942 178199 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4649860 178199 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
122180021 121556 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 528 7 2 7 4.9 O=C(NCC1COc2ccccc2O1)c1cc(-c2ccnc(Cl)c2)cnc1NCc1ccc2c(c1)OCC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586027 121556 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 528 7 2 7 4.9 O=C(NCC1COc2ccccc2O1)c1cc(-c2ccnc(Cl)c2)cnc1NCc1ccc2c(c1)OCC2 10.1016/j.bmcl.2015.04.040
11134880 99403 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 500 10 6 4 2.1 O=CN[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCNCC1 10.1021/jm020985q
CHEMBL282891 99403 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 500 10 6 4 2.1 O=CN[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCNCC1 10.1021/jm020985q
11846629 138794 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 419 7 3 7 3.1 Nc1nc(N)c(-c2ccc(NC(=O)C3CCCO3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL378118 138794 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 419 7 3 7 3.1 Nc1nc(N)c(-c2ccc(NC(=O)C3CCCO3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
11114279 98221 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 544 12 6 4 3.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(C)C 10.1021/jm020985q
CHEMBL274460 98221 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 544 12 6 4 3.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(C)C 10.1021/jm020985q
145952396 162979 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
CHEMBL4175534 162979 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
122178607 121318 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 592 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncc(F)cc2F)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581040 121318 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 592 11 2 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncc(F)cc2F)cc1 10.1016/j.bmcl.2014.11.031
156013219 177465 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639379 177465 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145957574 162277 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4164328 162277 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
11846463 139217 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 422 5 2 8 2.7 CCc1nc(N)nc(N)c1-c1ccc2c(c1)ncn2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
CHEMBL378909 139217 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 422 5 2 8 2.7 CCc1nc(N)nc(N)c1-c1ccc2c(c1)ncn2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
9890863 131966 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CC)CCN1C(=O)C(O)(c2ccccc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL369533 131966 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CC)CCN1C(=O)C(O)(c2ccccc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
44409864 75470 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 502 9 3 8 4.0 CN(Cc1ccccc1)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL204266 75470 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 502 9 3 8 4.0 CN(Cc1ccccc1)Cc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122180027 121562 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 566 8 2 7 5.2 CC(C)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586033 121562 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 566 8 2 7 5.2 CC(C)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
11430392 76695 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 431 6 3 7 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Cl)c1 10.1021/jm0510934
CHEMBL206588 76695 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 431 6 3 7 3.5 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Cl)c1 10.1021/jm0510934
57785737 113415 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 549 7 2 8 3.7 CN1CCCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319216 113415 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 549 7 2 8 3.7 CN1CCCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
44390871 64812 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2c(Cl)cccc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL182035 64812 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 503 7 2 4 4.0 CCN(CC)CCN1C(=O)[C@@](O)(c2c(Cl)cccc2Cl)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
70682037 75852 20 None 43 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 495 5 0 8 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048820 75852 20 None 43 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 495 5 0 8 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1 10.1016/j.bmcl.2012.05.024
156021297 178065 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647797 178065 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
90666040 109296 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 542 9 0 9 4.6 CCCOc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218913 109296 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 542 9 0 9 4.6 CCCOc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
90666026 109282 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 516 9 0 9 4.1 CCO[C@H](C)CN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218899 109282 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 516 9 0 9 4.1 CCO[C@H](C)CN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
16204021 84678 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 10 3 5 4.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(F)cc1 10.1021/jm070024h
CHEMBL222710 84678 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 10 3 5 4.9 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(F)cc1 10.1021/jm070024h
122180014 121549 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 539 9 2 8 5.8 CCCn1cc(-c2cnc(NCc3ccc4sccc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586020 121549 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 539 9 2 8 5.8 CCCn1cc(-c2cnc(NCc3ccc4sccc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
90666016 109272 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 481 5 0 9 2.9 Cc1ncccc1-c1nc2cn(-c3ccc(C#N)cc3)nc2c(=O)n1CC1CCCN(C2COC2)C1 10.1039/C2MD20340E
CHEMBL3218889 109272 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 481 5 0 9 2.9 Cc1ncccc1-c1nc2cn(-c3ccc(C#N)cc3)nc2c(=O)n1CC1CCCN(C2COC2)C1 10.1039/C2MD20340E
44389186 64585 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 379 7 1 5 4.8 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3OC)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL181739 64585 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 379 7 1 5 4.8 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3OC)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44338266 110306 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 523 11 1 6 4.3 CN(C)CCCN1C(=O)[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=O 10.1016/j.bmcl.2003.11.012
CHEMBL323974 110306 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 523 11 1 6 4.3 CN(C)CCCN1C(=O)[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=O 10.1016/j.bmcl.2003.11.012
70692602 75847 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 423 8 0 5 3.5 CCCOc1ccc(CN2CC3(CCN(C(=O)Cc4ccc(OC)cc4)CC3)C2)cn1 10.1016/j.bmcl.2012.05.024
CHEMBL2048815 75847 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 423 8 0 5 3.5 CCCOc1ccc(CN2CC3(CCN(C(=O)Cc4ccc(OC)cc4)CC3)C2)cn1 10.1016/j.bmcl.2012.05.024
11455251 161290 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 523 8 3 7 5.0 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3Br)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL412362 161290 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 523 8 3 7 5.0 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3Br)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
156021942 178199 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4649860 178199 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 475 8 3 5 1.1 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)C4CC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
16204037 137208 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccccc1Cn1c(Cc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL375150 137208 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 522 10 3 6 4.5 COc1ccccc1Cn1c(Cc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
11582836 62883 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 431 7 1 4 6.4 CCCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178463 62883 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 431 7 1 4 6.4 CCCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44389131 63432 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 485 6 1 4 7.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C(F)(F)F)c1 10.1016/j.bmcl.2004.11.075
CHEMBL179812 63432 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 485 6 1 4 7.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C(F)(F)F)c1 10.1016/j.bmcl.2004.11.075
122180025 121560 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 542 7 2 8 3.6 CC(=O)N1CC=C(c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)CC1 10.1016/j.bmcl.2015.04.040
CHEMBL3586031 121560 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 542 7 2 8 3.6 CC(=O)N1CC=C(c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)CC1 10.1016/j.bmcl.2015.04.040
122178612 121323 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 572 11 2 6 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc[n+]2[O-])cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581045 121323 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 572 11 2 6 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc[n+]2[O-])cc1 10.1016/j.bmcl.2014.11.031
16203237 96922 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 496 10 3 6 4.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccco1 10.1021/jm070024h
CHEMBL266199 96922 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 496 10 3 6 4.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccco1 10.1021/jm070024h
59446148 175025 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 840 21 10 9 1.3 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(CC1CCCCC1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4567800 175025 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 840 21 10 9 1.3 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(CC1CCCCC1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
46882152 5823 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 432 12 4 4 4.1 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(CCCN)c2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079302 5823 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 432 12 4 4 4.1 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(CCCN)c2)cc1 10.1016/j.bmcl.2009.08.076
11655355 74392 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)s3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL202642 74392 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3ccc(Cl)s3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
145952396 162979 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
CHEMBL4175534 162979 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C 10.1021/acs.jmedchem.8b00322
46882764 5599 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 375 9 3 3 4.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1077716 5599 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 375 9 3 3 4.2 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1016/j.bmcl.2009.08.076
16114290 137183 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 534 11 3 5 5.3 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL374992 137183 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 534 11 3 5 5.3 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
90666015 109271 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 483 7 0 9 3.2 COCCN1CCCC(Cn2c(-c3cccnc3C)nc3cn(-c4ccc(C#N)cc4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218888 109271 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 483 7 0 9 3.2 COCCN1CCCC(Cn2c(-c3cccnc3C)nc3cn(-c4ccc(C#N)cc4)nc3c2=O)C1 10.1039/C2MD20340E
44436831 151972 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 580 12 4 7 4.3 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL396681 151972 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 580 12 4 7 4.3 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
25262608 113436 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 492 6 2 7 3.8 O=C(NC(=O)c1ccccc1Cl)Nc1nc2ccc(S(=O)(=O)CCN3CCCC3)cc2s1 10.1021/jm500610n
CHEMBL3319279 113436 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 492 6 2 7 3.8 O=C(NC(=O)c1ccccc1Cl)Nc1nc2ccc(S(=O)(=O)CCN3CCCC3)cc2s1 10.1021/jm500610n
10918326 98944 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N(C)C 10.1021/jm020985q
CHEMBL279822 98944 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 516 10 5 4 2.8 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N(C)C 10.1021/jm020985q
16203918 84758 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 570 9 3 5 5.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1ccc(Br)cc1 10.1021/jm070024h
CHEMBL223239 84758 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 570 9 3 5 5.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1ccc(Br)cc1 10.1021/jm070024h
70696687 75844 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 446 7 0 6 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4cccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048812 75844 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 446 7 0 6 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4cccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
46882105 6319 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 460 12 4 4 4.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)CN)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1082044 6319 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 460 12 4 4 4.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)CN)cc2)cc1 10.1016/j.bmcl.2009.08.076
44446189 155350 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL403426 155350 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1 10.1016/j.bmcl.2007.10.113
44446157 94623 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 594 13 3 8 4.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](CC(=O)OCc2ccccc2)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252501 94623 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 594 13 3 8 4.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](CC(=O)OCc2ccccc2)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
44446148 155394 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL403683 155394 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
44410008 141226 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 9 2 7 4.2 CCc1nc(N)nc(N(CC)CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL383058 141226 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 9 2 7 4.2 CCc1nc(N)nc(N(CC)CC)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
59446143 81571 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 802 17 11 8 0.6 C[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O nan
CHEMBL2163448 81571 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 802 17 11 8 0.6 C[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O nan
59446143 81571 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 802 17 11 8 0.6 C[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1021/jm300557t
CHEMBL2163448 81571 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 802 17 11 8 0.6 C[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1021/jm300557t
44338221 8016 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 581 11 1 7 4.2 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=S)N1CCCN1CCOCC1 10.1016/j.bmcl.2003.11.012
CHEMBL109094 8016 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 581 11 1 7 4.2 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=S)N1CCCN1CCOCC1 10.1016/j.bmcl.2003.11.012
60195113 81578 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 787 17 9 7 2.5 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm300557t
CHEMBL2163467 81578 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 787 17 9 7 2.5 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/jm300557t
46882804 5791 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 446 11 4 4 4.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079045 5791 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 446 11 4 4 4.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
10864048 98360 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.6 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL275373 98360 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.6 CCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
156016110 177674 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 628 7 1 9 5.1 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccc(S(=O)(=O)C5CCN(C)CC5)cc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4642043 177674 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 628 7 1 9 5.1 CCOc1cc(Cl)c(-c2ccc(-c3nc4ccc(S(=O)(=O)C5CCN(C)CC5)cc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
156017268 177626 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641472 177626 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
59446118 174676 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)N(Cc1cccc2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4559602 174676 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)N(Cc1cccc2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
60195285 81583 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)N(Cc1cccc2ccccc12)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163473 81583 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)N(Cc1cccc2ccccc12)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44436868 146058 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 520 9 4 5 4.6 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1c1ccccc1)C1CCNCC1 10.1021/jm0704550
CHEMBL391922 146058 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 520 9 4 5 4.6 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1c1ccccc1)C1CCNCC1 10.1021/jm0704550
44394947 169199 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL440939 169199 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 551 9 1 6 7.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)cc1 10.1016/j.bmcl.2004.06.060
122180022 121557 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 504 7 2 9 2.8 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2CCOCC2)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
CHEMBL3586028 121557 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 504 7 2 9 2.8 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2CCOCC2)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
11751384 141481 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 453 9 3 6 4.6 Nc1nc(N)c(-c2ccc(NC(=O)CCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL384524 141481 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 453 9 3 6 4.6 Nc1nc(N)c(-c2ccc(NC(=O)CCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
122180026 121561 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 566 7 2 7 4.4 CC(=O)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586032 121561 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 566 7 2 7 4.4 CC(=O)N1[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmcl.2015.04.040
122182043 121972 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 580 7 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593632 121972 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 580 7 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCC5)c(C(=O)NC[C@H]4COc5ccccc5O4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
16204226 84770 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 486 12 3 5 5.1 CCCCCCn1c(Cc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL223323 84770 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 486 12 3 5 5.1 CCCCCCn1c(Cc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
118709472 113435 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 409 3 2 6 3.3 CS(=O)(=O)c1ccc2sc(NC(=O)NC(=O)c3ccccc3Cl)nc2c1 10.1021/jm500610n
CHEMBL3319277 113435 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 409 3 2 6 3.3 CS(=O)(=O)c1ccc2sc(NC(=O)NC(=O)c3ccccc3Cl)nc2c1 10.1021/jm500610n
46882196 5709 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 418 9 4 4 3.7 CCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078402 5709 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 418 9 4 4 3.7 CCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
44379303 12807 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 468 11 2 5 4.1 NCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1188529 12807 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 468 11 2 5 4.1 NCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL536706 12807 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 468 11 2 5 4.1 NCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(-c3ccccc3)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL2310893 209473 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)C(C)C 10.1021/jm0001727
44445614 169285 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 554 11 2 5 6.0 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2cccnc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL441567 169285 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 554 11 2 5 6.0 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2cccnc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
44445598 94347 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 565 9 3 5 6.5 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL250807 94347 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 565 9 3 5 6.5 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
145949381 162691 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4170865 162691 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
44436832 151974 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 548 11 4 5 4.9 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL396682 151974 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 548 11 4 5 4.9 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
44445626 97037 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 573 11 2 8 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL267197 97037 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 573 11 2 8 4.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
90666025 109281 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 516 9 0 9 4.1 CCO[C@@H](C)CN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218898 109281 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 516 9 0 9 4.1 CCO[C@@H](C)CN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
156012122 177357 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637980 177357 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156012122 177357 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4637980 177357 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156021297 178065 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4647797 178065 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 511 8 3 5 2.0 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)c4ccccc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
90666024 109280 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218897 109280 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
57422776 113417 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 559 7 2 8 3.3 C#Cc1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
CHEMBL3319218 113417 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 559 7 2 8 3.3 C#Cc1ccc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)CCCN4CCN(C)CC4)cc3s2)c1 10.1021/jm500610n
162657463 181016 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting methodDisplacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting method
ChEMBL 783 20 7 7 4.0 NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)C(N)=O 10.1016/j.ejmech.2016.07.078
CHEMBL4759415 181016 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting methodDisplacement of [125I-His9]-ghrelin from GHS-R1a (unknown origin) expressed in human HEK293 cells incubated for 20 mins by gamma scintillation counting method
ChEMBL 783 20 7 7 4.0 NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)C(N)=O 10.1016/j.ejmech.2016.07.078
44409990 76488 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 481 12 3 7 5.2 CCCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205995 76488 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 481 12 3 7 5.2 CCCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122180024 121559 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 530 7 2 9 3.4 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2C[C@@H]3CC[C@H](C2)O3)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
CHEMBL3586030 121559 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 530 7 2 9 3.4 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2C[C@@H]3CC[C@H](C2)O3)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
44409758 75945 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 411 6 3 7 3.4 CC(C)c1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205374 75945 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 411 6 3 7 3.4 CC(C)c1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
122182190 121983 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
CHEMBL3593815 121983 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 507 7 3 6 4.7 Cc1ccc(CNC(=O)c2cc(C#CC(C)(C)O)cnc2NCc2ccc3c(c2)OCO3)cc1C(F)F 10.1016/j.bmc.2015.05.047
44409684 140860 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 474 8 4 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL382033 140860 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 474 8 4 8 3.9 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
16113003 94718 2 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 617 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)c(OC)c1 10.1021/jm701292s
CHEMBL253126 94718 2 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 617 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)c(OC)c1 10.1021/jm701292s
16113003 94718 2 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 617 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)c(OC)c1 10.1021/jm0704550
CHEMBL253126 94718 2 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 617 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)c(OC)c1 10.1021/jm0704550
122182047 121976 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593636 121976 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
90666030 109286 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 486 7 0 8 4.3 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218903 109286 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 486 7 0 8 4.3 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC(C)C)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
11605333 76696 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 475 6 3 7 3.6 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Br)c1 10.1021/jm0510934
CHEMBL206589 76696 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 475 6 3 7 3.6 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)c(Br)c1 10.1021/jm0510934
122182046 121975 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 586 8 2 6 5.6 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCC3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593635 121975 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 586 8 2 6 5.6 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCC3)cc1Cl 10.1016/j.bmc.2015.05.047
11281346 75989 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 411 8 3 6 4.6 Nc1nc(N)c(-c2ccc(NCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL205568 75989 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 411 8 3 6 4.6 Nc1nc(N)c(-c2ccc(NCc3ccccc3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
145949381 162691 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4170865 162691 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
16204145 136527 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 492 9 3 5 4.5 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1ccccc1 10.1021/jm070024h
CHEMBL373772 136527 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 492 9 3 5 4.5 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1Cc1ccccc1 10.1021/jm070024h
90666036 109292 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 479 8 0 8 3.7 COc1cccc(-n2cc3nc(CC(C)C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218909 109292 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 479 8 0 8 3.7 COc1cccc(-n2cc3nc(CC(C)C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
44338235 109635 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 546 7 3 6 4.1 O=C1[C@H](Cc2c[nH]c3ccccc23)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=O)N1C1CCNCC1 10.1016/j.bmcl.2003.11.012
CHEMBL322499 109635 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 546 7 3 6 4.1 O=C1[C@H](Cc2c[nH]c3ccccc23)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=O)N1C1CCNCC1 10.1016/j.bmcl.2003.11.012
156016392 177622 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641386 177622 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156017268 177626 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641472 177626 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 497 8 3 5 1.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145958317 162289 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164531 162289 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145949880 162767 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4172217 162767 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
145950963 162782 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4172411 162782 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
156016392 177622 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641386 177622 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
44445608 154991 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 554 11 2 5 6.0 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL401468 154991 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 554 11 2 5 6.0 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
59446116 81569 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 777 17 9 8 0.8 C[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)N(Cc1ccccc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1021/jm300557t
CHEMBL2163439 81569 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 777 17 9 8 0.8 C[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)N(Cc1ccccc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1021/jm300557t
23631387 93237 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 409 4 0 4 5.1 Cc1nc2ccc(-c3ccc(Cl)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1039/C2MD20340E
CHEMBL244936 93237 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 409 4 0 4 5.1 Cc1nc2ccc(-c3ccc(Cl)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1039/C2MD20340E
90666038 109294 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1ccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)cc1 10.1039/C2MD20340E
CHEMBL3218911 109294 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1ccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)cc1 10.1039/C2MD20340E
44421230 84762 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 546 8 3 5 5.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1-c1ccc(Cl)c(Cl)c1 10.1021/jm070024h
CHEMBL223269 84762 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 546 8 3 5 5.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1-c1ccc(Cl)c(Cl)c1 10.1021/jm070024h
156018460 177853 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 468 5 1 7 4.6 CCOc1cc(Cl)c(-c2ncc(-c3nc4ccccc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
CHEMBL4644587 177853 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 468 5 1 7 4.6 CCOc1cc(Cl)c(-c2ncc(-c3nc4ccccc4s3)c(=O)[nH]2)cc1N1CCOCC1 10.1016/j.bmcl.2020.126953
145950963 162782 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4172411 162782 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
11618705 166914 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 423 6 1 4 5.3 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL428698 166914 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 423 6 1 4 5.3 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)CC1 10.1016/j.bmcl.2004.06.060
44436842 146913 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCCCN2)cc1 10.1021/jm0704550
CHEMBL392592 146913 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCCCN2)cc1 10.1021/jm0704550
CHEMBL509976 215557 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)N)C(N)=O 10.1074/jbc.m609796200
CHEMBL450217 213940 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in COS-7 cells incubated for 3 hrsDisplacement of [35S]MK677 from human ghrelin receptor expressed in COS-7 cells incubated for 3 hrs
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm300414b
CHEMBL450217 213940 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1c[nH]c2ccccc12)C(N)=O 10.1074/jbc.m609796200
10984270 98479 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 530 11 6 4 3.3 CC(C)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL276137 98479 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 530 11 6 4 3.3 CC(C)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
44436884 91523 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 565 11 5 7 3.1 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL240522 91523 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 565 11 5 7 3.1 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL444131 213906 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None NC(=O)CNC(=O)CNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](N)Cc1c[nH]c2ccccc12 10.1074/jbc.m609796200
60195020 81576 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 835 21 10 8 1.8 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163465 81576 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 835 21 10 8 1.8 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)CN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
59446112 172950 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 840 21 10 9 1.3 C[C@H](NC(=O)N(CC1CCCCC1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4517723 172950 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 840 21 10 9 1.3 C[C@H](NC(=O)N(CC1CCCCC1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL422461 213263 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm0001727
16114010 136258 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 613 10 4 5 6.5 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(Cl)c(Cl)c1 10.1021/jm070024h
CHEMBL373392 136258 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 613 10 4 5 6.5 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(Cl)c(Cl)c1 10.1021/jm070024h
16203349 166266 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 12 3 6 4.9 COc1ccc(CCn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL427076 166266 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 12 3 6 4.9 COc1ccc(CCn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
11531313 62474 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 394 7 1 6 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3[N+](=O)[O-])noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178137 62474 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 394 7 1 6 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3[N+](=O)[O-])noc2C)cc1 10.1016/j.bmcl.2004.11.075
44389283 62915 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 403 5 1 4 5.7 CCN(C)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178494 62915 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 403 5 1 4 5.7 CCN(C)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
122180019 121554 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586025 121554 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 513 8 2 9 3.9 CCn1cc(-c2cnc(NCc3ccc4c(c3)OCO4)c(C(=O)NC[C@@H]3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL447282 213926 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
ChEMBL None None None CCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm8014519
145958317 162289 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4164531 162289 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
16114008 84817 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccccc1Cn1c(CCc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL223532 84817 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1ccccc1Cn1c(CCc2ccccc2)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
16112910 136352 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 552 11 3 7 4.6 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
CHEMBL373507 136352 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 552 11 3 7 4.6 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
16112910 136352 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 552 11 3 7 4.6 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL373507 136352 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 552 11 3 7 4.6 COc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
44436882 145991 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 10 4 6 4.2 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1Cc1ccco1)C1CCNCC1 10.1021/jm0704550
CHEMBL391859 145991 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 10 4 6 4.2 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1Cc1ccco1)C1CCNCC1 10.1021/jm0704550
145949880 162767 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4172217 162767 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 390 6 3 3 2.3 CN(C)CCNC(=O)[C@@H]1c2ccccc2C[C@H]1NC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.8b00322
122180024 121559 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 530 7 2 9 3.4 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2C[C@@H]3CC[C@H](C2)O3)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
CHEMBL3586030 121559 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 530 7 2 9 3.4 O=C(NC[C@H]1COc2ccccc2O1)c1cc(N2C[C@@H]3CC[C@H](C2)O3)cnc1NCc1ccc2c(c1)OCO2 10.1016/j.bmcl.2015.04.040
46882154 5829 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 390 7 4 4 2.9 CCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079323 5829 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 390 7 4 4 2.9 CCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
59446145 81570 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 793 19 11 8 0.8 C[C@H](N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163444 81570 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 793 19 11 8 0.8 C[C@H](N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
59446145 81570 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 793 19 11 8 0.8 C[C@H](N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163444 81570 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 793 19 11 8 0.8 C[C@H](N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NNC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
11699004 66173 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 501 9 1 5 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL184429 66173 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 501 9 1 5 6.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2CCCO2)cc1 10.1016/j.bmcl.2004.06.060
11537800 75538 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 361 6 3 6 3.7 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)=O)cc2)cc1 10.1021/jm0510934
CHEMBL204564 75538 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 361 6 3 6 3.7 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(C(C)=O)cc2)cc1 10.1021/jm0510934
16203236 166238 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 512 10 3 6 4.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1cccs1 10.1021/jm070024h
CHEMBL426905 166238 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 512 10 3 6 4.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1cccs1 10.1021/jm070024h
10207327 67041 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
CHEMBL18725 67041 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
44445603 154956 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 572 11 2 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccncc2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL401259 154956 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 572 11 2 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccncc2)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL502208 214127 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1074/jbc.m609796200
16113583 161727 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 469 8 4 5 3.7 Cn1c(CCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL413856 161727 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 469 8 4 5 3.7 Cn1c(CCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
90665849 109249 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 508 7 0 7 5.5 COCCN1CCC[C@@H](Cn2c(-c3ccccc3C)nc3nc(-c4ccc(Cl)cc4)sc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218649 109249 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 508 7 0 7 5.5 COCCN1CCC[C@@H](Cn2c(-c3ccccc3C)nc3nc(-c4ccc(Cl)cc4)sc3c2=O)C1 10.1039/C2MD20340E
70696688 75850 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 487 9 0 6 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cn1 10.1016/j.bmcl.2012.05.024
CHEMBL2048818 75850 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 487 9 0 6 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cn1 10.1016/j.bmcl.2012.05.024
44436816 91776 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 12 4 6 3.9 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CCN)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL241242 91776 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 524 12 4 6 3.9 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CCN)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
10984270 98479 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 530 11 6 4 3.3 CC(C)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
CHEMBL276137 98479 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 530 11 6 4 3.3 CC(C)CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm020985q
44301387 11232 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1179088 11232 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL59572 11232 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
11692087 62962 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL178610 62962 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.06.060
122178610 121321 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(N)n2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581043 121321 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 571 11 3 7 5.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cccc(N)n2)cc1 10.1016/j.bmcl.2014.11.031
16113695 137002 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm701292s
CHEMBL374643 137002 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm701292s
16113695 137002 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL374643 137002 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
16113695 137002 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL374643 137002 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
16113695 137002 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm0704550
CHEMBL374643 137002 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm0704550
44436888 153032 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 565 11 3 6 5.0 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCOCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL397593 153032 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 565 11 3 6 5.0 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCOCC3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
11692087 62962 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178610 62962 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 517 9 1 6 6.4 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)cc1 10.1016/j.bmcl.2004.11.075
44409809 75036 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 10 3 7 4.4 CCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203578 75036 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 453 10 3 7 4.4 CCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44409989 165802 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 467 11 3 7 4.8 CCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL424860 165802 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 467 11 3 7 4.8 CCCCCCCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL105462 208445 38 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
90666018 109274 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 488 8 0 9 3.3 COCCN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
CHEMBL3218891 109274 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 488 8 0 9 3.3 COCCN1CCC[C@H](Cn2c(-c3cccnc3C)nc3cn(-c4cccc(OC)c4)nc3c2=O)C1 10.1039/C2MD20340E
11612155 140984 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3csc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
CHEMBL382375 140984 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 451 8 3 7 5.4 Nc1nc(N)c(-c2ccc(NCc3csc(Cl)c3)cc2)c(COCc2ccccc2)n1 10.1021/jm0510934
118722878 116171 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 494 5 2 4 4.8 CN1CCN([C@@H](C(=O)NNc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2Cl)CC1 10.1021/jm5003183
CHEMBL3358451 116171 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human ghrelin receptor by FLIPR assayAntagonist activity against human ghrelin receptor by FLIPR assay
ChEMBL 494 5 2 4 4.8 CN1CCN([C@@H](C(=O)NNc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ccccc2Cl)CC1 10.1021/jm5003183
16114097 79128 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCCNC2)c(OC)c1 10.1021/jm0704550
CHEMBL2113321 79128 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCCNC2)c(OC)c1 10.1021/jm0704550
122182189 121982 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593814 121982 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 548 8 3 7 4.3 COc1ccc(CNC(=O)c2cc(C#CC(C)(C)NC(C)=O)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
25260901 113453 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 577 5 2 9 3.6 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319405 113453 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 577 5 2 9 3.6 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc(N5CCOCC5)ccc4Cl)sc3c2)CC1 10.1021/jm500610n
122180021 121556 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 528 7 2 7 4.9 O=C(NCC1COc2ccccc2O1)c1cc(-c2ccnc(Cl)c2)cnc1NCc1ccc2c(c1)OCC2 10.1016/j.bmcl.2015.04.040
CHEMBL3586027 121556 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 528 7 2 7 4.9 O=C(NCC1COc2ccccc2O1)c1cc(-c2ccnc(Cl)c2)cnc1NCc1ccc2c(c1)OCC2 10.1016/j.bmcl.2015.04.040
11179347 77324 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 490 9 2 8 4.0 CS(=O)(=O)c1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL208477 77324 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 490 9 2 8 4.0 CS(=O)(=O)c1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
44445593 154763 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 552 11 3 7 4.6 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)C(C)(C)N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
CHEMBL400174 154763 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 552 11 3 7 4.6 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)C(C)(C)N)c2c[nH]c3ccccc23)c(OC)c1 10.1021/jm701292s
16203569 141708 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
CHEMBL385803 141708 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
90666034 109290 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.7 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCOC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218907 109290 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.7 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCOC5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL449590 213939 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cellsDisplacement of [35S]MK677 from human ghrelin receptor expressed in african green monkey COS7 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CC(=O)O)C(N)=O 10.1074/jbc.m609796200
121879 2222 24 None - 1 Rat 7.2 pIC50 = 7.2 Binding
Inhibition against rat growth hormone secretagogue (GHS) receptorInhibition against rat growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
5868 2222 24 None - 1 Rat 7.2 pIC50 = 7.2 Binding
Inhibition against rat growth hormone secretagogue (GHS) receptorInhibition against rat growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
CHEMBL308716 2222 24 None - 1 Rat 7.2 pIC50 = 7.2 Binding
Inhibition against rat growth hormone secretagogue (GHS) receptorInhibition against rat growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
11568561 169530 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 447 7 1 5 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(OC)c1 10.1016/j.bmcl.2004.11.075
CHEMBL443560 169530 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 447 7 1 5 6.1 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(OC)c1 10.1016/j.bmcl.2004.11.075
44338246 98826 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 563 11 1 6 5.2 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
CHEMBL278909 98826 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 563 11 1 6 5.2 O=C1[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C(=O)N1CCCN1CCCCC1 10.1016/j.bmcl.2003.11.012
CHEMBL105462 208445 38 None - 1 Human 5.2 pIC50 = 5.2 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/s0960-894x(99)00584-3
44409767 157218 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 437 8 3 7 3.9 CCc1nc(N)nc(NC2CC2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL407647 157218 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 437 8 3 7 3.9 CCc1nc(N)nc(NC2CC2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
44445612 97011 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 565 10 3 5 5.9 O=C(Cc1ccccn1)N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm701292s
CHEMBL266964 97011 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 565 10 3 5 5.9 O=C(Cc1ccccn1)N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccccc1 10.1021/jm701292s
44410003 76152 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 468 10 4 8 3.5 CC(C)CCNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205794 76152 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 468 10 4 8 3.5 CC(C)CCNCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
16203569 141708 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL385803 141708 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 566 12 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL18872 209035 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(C)(C)N)C(N)=O 10.1021/jm300557t
46882106 5830 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 418 11 4 4 3.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(CCN)c2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079340 5830 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 418 11 4 4 3.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(CCN)c2)cc1 10.1016/j.bmcl.2009.08.076
44436876 146994 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 580 11 4 7 4.6 COc1ccc(N2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
CHEMBL392663 146994 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 580 11 4 7 4.6 COc1ccc(N2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1 10.1021/jm0704550
121879 2222 24 None - 1 Pig 7.2 pIC50 = 7.2 Binding
Inhibition against pig growth hormone secretagogue (GHS) receptorInhibition against pig growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
5868 2222 24 None - 1 Pig 7.2 pIC50 = 7.2 Binding
Inhibition against pig growth hormone secretagogue (GHS) receptorInhibition against pig growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
CHEMBL308716 2222 24 None - 1 Pig 7.2 pIC50 = 7.2 Binding
Inhibition against pig growth hormone secretagogue (GHS) receptorInhibition against pig growth hormone secretagogue (GHS) receptor
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm0309452
156010733 177056 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633062 177056 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145962494 162050 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160705 162050 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
145950201 162918 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174476 162918 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
44409832 76381 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 398 6 4 8 1.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205955 76381 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 398 6 4 8 1.8 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CN)cc2)cc1 10.1016/j.bmcl.2006.01.012
16204237 84868 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 574 10 3 5 6.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(Cl)c(Cl)c1 10.1021/jm070024h
CHEMBL223638 84868 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 574 10 3 5 6.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(Cl)c(Cl)c1 10.1021/jm070024h
16204343 137166 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 635 12 4 5 7.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1CC(c1ccccc1)c1ccccc1 10.1021/jm070024h
CHEMBL374918 137166 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 635 12 4 5 7.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1CC(c1ccccc1)c1ccccc1 10.1021/jm070024h
122178613 121324 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 625 12 2 7 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(N3CCCC3)cn2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581046 121324 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 625 12 2 7 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccc(N3CCCC3)cn2)cc1 10.1016/j.bmcl.2014.11.031
57422749 113412 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 492 4 2 7 3.8 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319213 113412 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 492 4 2 7 3.8 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
44410007 76398 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 438 8 4 8 2.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL205963 76398 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 438 8 4 8 2.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNC3CC3)cc2)cc1 10.1016/j.bmcl.2006.01.012
118718706 115353 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL3350011 115353 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
89768546 148993 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of ghrelin receptor (unknown origin) by radioligand binding assayInhibition of ghrelin receptor (unknown origin) by radioligand binding assay
ChEMBL 438 4 2 5 5.5 Cc1nnc2sc(C(=O)NCc3ccc(S(F)(F)(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
CHEMBL3942511 148993 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of ghrelin receptor (unknown origin) by radioligand binding assayInhibition of ghrelin receptor (unknown origin) by radioligand binding assay
ChEMBL 438 4 2 5 5.5 Cc1nnc2sc(C(=O)NCc3ccc(S(F)(F)(F)(F)F)cc3)c(N)c2c1C 10.1016/j.bmcl.2016.11.086
16114011 138113 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 563 10 4 5 5.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(F)cc1 10.1021/jm070024h
CHEMBL376736 138113 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 563 10 4 5 5.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(F)cc1 10.1021/jm070024h
11349789 78744 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 389 7 3 6 3.4 Nc1nc(N)c(-c2ccc(NC(=O)C3CC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL211265 78744 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 389 7 3 6 3.4 Nc1nc(N)c(-c2ccc(NC(=O)C3CC3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
16112909 144256 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 561 10 4 6 5.0 COc1ccc(Cn2c(Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL390503 144256 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 561 10 4 6 5.0 COc1ccc(Cn2c(Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
44378837 12989 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 484 11 2 5 3.6 NCCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1189851 12989 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 484 11 2 5 3.6 NCCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL539575 12989 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 484 11 2 5 3.6 NCCCCCCNC(=O)Cn1c(CCc2ccccc2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
44445597 94487 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 540 10 2 5 6.1 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL251640 94487 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 540 10 2 5 6.1 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
11176805 77305 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 391 7 3 6 4.5 CC(C)(C)CNc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm0510934
CHEMBL208374 77305 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 391 7 3 6 4.5 CC(C)(C)CNc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm0510934
156010733 177056 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4633062 177056 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 520 8 3 6 0.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
46882153 5828 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 528 13 4 4 5.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NCC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1079322 5828 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 528 13 4 4 5.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)NCC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2009.08.076
145950201 162918 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4174476 162918 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
46882239 5752 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 7 4 4 4.7 Cc1cccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)c1 10.1016/j.bmcl.2009.08.076
CHEMBL1078700 5752 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 7 4 4 4.7 Cc1cccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)c1 10.1016/j.bmcl.2009.08.076
1221269 122008 12 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL359530 122008 12 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44446177 94618 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252448 94618 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1016/j.bmcl.2007.10.113
16114289 98637 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCNC2)cc1 10.1021/jm0704550
CHEMBL277376 98637 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 562 11 3 6 5.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCNC2)cc1 10.1021/jm0704550
11538533 74972 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm060461g
CHEMBL203280 74972 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm060461g
10415364 126741 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against mouse Growth hormone secretagogue receptorInhibitory concentration against mouse Growth hormone secretagogue receptor
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL365294 126741 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against mouse Growth hormone secretagogue receptorInhibitory concentration against mouse Growth hormone secretagogue receptor
ChEMBL 557 9 1 6 6.5 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCc2ccc3c(c2)OCO3)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL263544 210552 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0001727
122180023 121558 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 530 7 2 8 3.8 C[C@H]1CN(c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)C[C@@H](C)O1 10.1016/j.bmcl.2015.04.040
CHEMBL3586029 121558 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 530 7 2 8 3.8 C[C@H]1CN(c2cnc(NCc3ccc4c(c3)OCC4)c(C(=O)NC[C@H]3COc4ccccc4O3)c2)C[C@@H](C)O1 10.1016/j.bmcl.2015.04.040
118709507 113456 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 547 4 2 8 3.8 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc5c(cc4Cl)CCN5C)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319408 113456 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 547 4 2 8 3.8 CN1CCC(S(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cc5c(cc4Cl)CCN5C)sc3c2)CC1 10.1021/jm500610n
90666011 109267 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 471 6 0 7 4.7 COc1ccc(-n2cc3nc(-c4ccccc4C)n(CC4CCCN(C(C)C)C4)c(=O)c3n2)cc1 10.1039/C2MD20340E
CHEMBL3218884 109267 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 471 6 0 7 4.7 COc1ccc(-n2cc3nc(-c4ccccc4C)n(CC4CCCN(C(C)C)C4)c(=O)c3n2)cc1 10.1039/C2MD20340E
11538533 74972 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
CHEMBL203280 74972 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
44409998 138511 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 413 7 3 8 2.5 COCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL377515 138511 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 413 7 3 8 2.5 COCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
90666021 109277 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218894 109277 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 514 7 0 9 3.9 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(CC5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
11453509 76149 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 441 9 3 7 4.6 COc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL205784 76149 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 441 9 3 7 4.6 COc1ccc(CNc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
44445610 161699 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 595 11 3 6 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL413608 161699 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 595 11 3 6 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
23648249 79133 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 557 9 4 5 5.4 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1)C1CCNCC1 10.1021/jm0704550
CHEMBL2113326 79133 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 557 9 4 5 5.4 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1)C1CCNCC1 10.1021/jm0704550
11178309 79872 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 445 8 3 7 4.3 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL212415 79872 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 445 8 3 7 4.3 Nc1nc(N)c(-c2ccc(NC(=O)Cc3ccsc3)cc2)c(COCc2ccccc2)n1 10.1021/jm060461g
CHEMBL3578018 211746 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
CHEMBL3578018 211746 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
44445613 94158 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 512 9 2 5 5.4 O=C(Cc1ccccn1)N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1-c1ccccc1 10.1021/jm701292s
CHEMBL249662 94158 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 512 9 2 5 5.4 O=C(Cc1ccccn1)N[C@H](c1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1-c1ccccc1 10.1021/jm701292s
16204229 84288 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
CHEMBL221569 84288 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 545 10 4 5 5.2 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(Cc2ccccc2)n1CCc1c[nH]c2ccccc12 10.1021/jm070024h
44409867 76712 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 473 8 3 7 5.0 CCc1nc(N)nc(Nc2ccccc2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL206672 76712 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 473 8 3 7 5.0 CCc1nc(N)nc(Nc2ccccc2)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
145962494 162050 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
CHEMBL4160705 162050 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 446 4 2 5 2.4 CN1CCCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1 10.1021/acs.jmedchem.8b00322
44389215 63048 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccc(Cl)cc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL178838 63048 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 383 6 1 4 5.4 CCN(CC)c1ccc(NC(=O)c2c(-c3ccc(Cl)cc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
11211892 80187 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 405 8 3 6 4.0 CC(C)CC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
CHEMBL213703 80187 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 405 8 3 6 4.0 CC(C)CC(=O)Nc1ccc(-c2c(N)nc(N)nc2COCc2ccccc2)cc1 10.1021/jm060461g
122180015 121550 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 523 9 2 8 5.3 CCCn1cc(-c2cnc(NCc3ccc4occc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586021 121550 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 523 9 2 8 5.3 CCCn1cc(-c2cnc(NCc3ccc4occc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
59446138 81592 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1cccc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163482 81592 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1cccc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
59446138 81592 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1cccc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163482 81592 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 884 21 10 9 2.1 C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)NN(Cc1cccc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
59446127 173012 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)N(CCc1ccccc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4518972 173012 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)N(CCc1ccccc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
60195286 81584 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)N(CCc1ccccc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163474 81584 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 848 22 10 9 1.0 C[C@H](NC(=O)N(CCc1ccccc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
10207327 67041 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
CHEMBL18725 67041 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL 502 10 6 4 2.5 CNC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)NC(C)=O 10.1021/jm020985q
16112911 84700 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 619 13 4 7 5.6 COc1ccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
CHEMBL222835 84700 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 619 13 4 7 5.6 COc1ccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1021/jm070024h
5311280 81580 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 1035 25 11 10 2.4 Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)[C@@H]1Cc2cccc3c2N1C(=O)[C@@H](N)CC3)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163470 81580 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 1035 25 11 10 2.4 Cc1[nH]c2ccccc2c1C[C@@H](NC(=O)[C@@H]1Cc2cccc3c2N1C(=O)[C@@H](N)CC3)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
44389243 64553 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 557 7 1 6 6.2 O=C(Nc1ccccc1C(=O)N1CCCCC1)c1c(-c2c(Cl)cccc2Cl)noc1CCC1OCCCO1 10.1016/j.bmcl.2004.11.075
CHEMBL181619 64553 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 557 7 1 6 6.2 O=C(Nc1ccccc1C(=O)N1CCCCC1)c1c(-c2c(Cl)cccc2Cl)noc1CCC1OCCCO1 10.1016/j.bmcl.2004.11.075
23648232 91214 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 506 11 3 5 4.5 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/jm0704550
CHEMBL240179 91214 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 506 11 3 5 4.5 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/jm0704550
44445616 161846 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 595 11 3 6 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccncc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL414930 161846 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 595 11 3 6 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccncc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
118709471 113433 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 361 3 2 5 3.9 COc1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319275 113433 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 361 3 2 5 3.9 COc1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
44390889 64393 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 465 8 2 5 2.7 CCN(CC)CCN1C(=O)[C@@](O)(c2cccc(OC)c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL181313 64393 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 465 8 2 5 2.7 CCN(CC)CCN1C(=O)[C@@](O)(c2cccc(OC)c2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
46882270 5785 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 7 4 4 4.7 Cc1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078960 5785 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 452 7 4 4 4.7 Cc1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
156016696 177606 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641201 177606 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL3578016 211744 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
CHEMBL2163348 209301 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL2163348 209301 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
16113800 137787 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1cccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL375972 137787 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 536 11 3 6 4.7 COc1cccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1 10.1021/jm070024h
CHEMBL3578016 211744 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
156013130 177478 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639514 177478 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
156016696 177606 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4641201 177606 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 478 8 3 5 0.4 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N(C)C)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
145950877 162971 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4175360 162971 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
44358041 161307 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 1724 59 24 24 -8.1 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O)C(C)C 10.1021/jm0001727
91931457 161307 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 1724 59 24 24 -8.1 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O)C(C)C 10.1021/jm0001727
CHEMBL412565 161307 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL 1724 59 24 24 -8.1 CCCCCCCC(=O)NC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O)C(C)C 10.1021/jm0001727
57422810 177637 4 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 602 7 2 10 4.4 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1016/j.bmcl.2020.126953
CHEMBL4641579 177637 4 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 602 7 2 10 4.4 CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(S(=O)(=O)C4CCN(C)CC4)cc3s2)cc1-n1cccn1 10.1016/j.bmcl.2020.126953
16113246 94648 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL252643 94648 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
11846624 77887 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 490 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(C1CCCC1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
CHEMBL209443 77887 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]ghrelin binding to GHS receptor in CHO-K cellsInhibition of [125I]ghrelin binding to GHS receptor in CHO-K cells
ChEMBL 490 6 2 8 4.3 CCc1nc(N)nc(N)c1-c1ccc2c(c1)nc(C1CCCC1)n2Cc1ccc(S(C)(=O)=O)cc1 10.1021/jm060461g
46882272 5778 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 480 8 4 4 5.5 CC(C)c1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078900 5778 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 480 8 4 4 5.5 CC(C)c1ccc(NC(=O)Nc2ccc(S(=O)(=O)Nc3ccc(CC(C)(C)N)cc3)cc2)cc1 10.1016/j.bmcl.2009.08.076
9987037 12000 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1183385 12000 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL294324 12000 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 564 12 2 7 2.5 CCCCCCCC(=O)OC[C@@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
56942537 125174 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 551 12 2 6 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)OCC(C)C)cc1 nan
CHEMBL3645262 125174 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Competitive Binding Assay: Competitive binding assay using ghrelin receptor.Competitive Binding Assay: Competitive binding assay using ghrelin receptor.
ChEMBL 551 12 2 6 6.3 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)OCC(C)C)cc1 nan
57422761 113413 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 510 10 3 8 3.3 COCCNCCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319214 113413 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 510 10 3 8 3.3 COCCNCCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
57422760 113410 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 480 7 2 7 3.6 CN(C)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
CHEMBL3319211 113410 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 480 7 2 7 3.6 CN(C)CCCS(=O)(=O)c1ccc2nc(NC(=O)NC(=O)c3ccccc3Cl)sc2c1 10.1021/jm500610n
57422791 113425 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 601 8 2 10 3.5 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cccc(-n5cccn5)c4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319226 113425 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 601 8 2 10 3.5 CN1CCN(CCCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4cccc(-n5cccn5)c4Cl)sc3c2)CC1 10.1021/jm500610n
44445619 154653 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 541 10 2 5 6.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL399650 154653 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 541 10 2 5 6.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccc2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
16113469 137477 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 559 11 4 5 5.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
CHEMBL375408 137477 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 559 11 4 5 5.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1CCc1ccccc1 10.1021/jm070024h
122182045 121974 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 554 9 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCO5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593634 121974 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 554 9 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCO5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
44446175 94958 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 566 13 3 7 4.7 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL254741 94958 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 566 13 3 7 4.7 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2007.10.113
10994861 67241 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 514 9 6 4 2.5 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCNCC1 10.1021/jm020985q
CHEMBL18815 67241 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 514 9 6 4 2.5 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCNCC1 10.1021/jm020985q
10984260 168329 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 529 9 7 5 1.6 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1(N)CCNCC1 10.1021/jm020985q
CHEMBL434391 168329 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligandBinding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand
ChEMBL 529 9 7 5 1.6 CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1(N)CCNCC1 10.1021/jm020985q
59446135 81586 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 859 21 12 9 0.7 NCCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O nan
CHEMBL2163476 81586 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 859 21 12 9 0.7 NCCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O nan
59446135 81586 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 859 21 12 9 0.7 NCCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1021/jm300557t
CHEMBL2163476 81586 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 859 21 12 9 0.7 NCCCC[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)NNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(N)=O 10.1021/jm300557t
59446154 81573 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 858 19 10 8 2.0 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(N)=O nan
CHEMBL2163453 81573 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 858 19 10 8 2.0 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(N)=O nan
59446154 81573 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 858 19 10 8 2.0 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(N)=O 10.1021/jm300557t
CHEMBL2163453 81573 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 858 19 10 8 2.0 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](C)C(N)=O 10.1021/jm300557t
44446178 155099 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL402023 155099 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2007.10.113
753168 123213 40 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 349 6 1 4 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL361366 123213 40 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 349 6 1 4 4.7 CCN(CC)c1ccc(NC(=O)c2c(-c3ccccc3)noc2C)cc1 10.1016/j.bmcl.2004.11.075
44338253 9255 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 539 11 1 6 4.4 CN(C)CCCN1C(=O)[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=S 10.1016/j.bmcl.2003.11.012
CHEMBL110900 9255 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cellsInhibition of ghrelin binding to Growth hormone secretagogue receptor expressed in BHK cells
ChEMBL 539 11 1 6 4.4 CN(C)CCCN1C(=O)[C@H](CCc2ccccc2)N(Cc2ccc(-c3ccccc3-c3nn[nH]n3)cc2)C1=S 10.1016/j.bmcl.2003.11.012
44301512 11990 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 566 13 3 8 1.0 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@@H](N)CO)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL1183340 11990 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 566 13 3 8 1.0 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@@H](N)CO)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
CHEMBL291333 11990 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL 566 13 3 8 1.0 CCCCCCCC(=O)OC[C@@H](NC(=O)[C@@H](N)CO)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12 10.1016/s0960-894x(01)00324-9
16113799 168689 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
CHEMBL436849 168689 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 605 12 4 7 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c(OC)c1 10.1016/j.bmcl.2007.10.113
11166495 75521 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 437 8 2 7 4.5 N#Cc1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
CHEMBL204474 75521 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 437 8 2 7 4.5 N#Cc1ccc(COc2ccc(-c3c(N)nc(N)nc3COCc3ccccc3)cc2)cc1 10.1021/jm0510934
25262772 113438 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 521 6 2 8 2.9 CN1CCN(CCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
CHEMBL3319281 113438 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting methodDisplacement of [125I]human ghrelin from human GHS-R1a expressed in HEK cell membranes after 60 mins by gamma counting method
ChEMBL 521 6 2 8 2.9 CN1CCN(CCS(=O)(=O)c2ccc3nc(NC(=O)NC(=O)c4ccccc4Cl)sc3c2)CC1 10.1021/jm500610n
44390869 122316 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc(Cl)cc2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
CHEMBL359922 122316 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparationInhibition of [125I]ghrelin binding to human recombinant ghrelin receptor membrane preparation
ChEMBL 469 7 2 4 3.4 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc(Cl)cc2)c2c1cc(C(N)=O)cc2C(F)(F)F 10.1016/j.bmcl.2005.02.042
156013130 177478 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
CHEMBL4639514 177478 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting methodDisplacement of [His[125I]]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method
ChEMBL 505 8 3 6 0.7 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)C4CCOCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1 10.1021/acs.jmedchem.0c00828
122180014 121549 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 539 9 2 8 5.8 CCCn1cc(-c2cnc(NCc3ccc4sccc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586020 121549 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to ghrelin receptor (unknown origin)Binding affinity to ghrelin receptor (unknown origin)
ChEMBL 539 9 2 8 5.8 CCCn1cc(-c2cnc(NCc3ccc4sccc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
122178601 121311 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cncc(Br)c2)cc1 10.1016/j.bmcl.2014.11.031
CHEMBL3581034 121311 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assayDisplacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
ChEMBL 634 11 2 6 6.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cncc(Br)c2)cc1 10.1016/j.bmcl.2014.11.031
16202767 84967 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 506 9 3 5 4.8 Cc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
CHEMBL223810 84967 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 506 9 3 5 4.8 Cc1ccc(Cn2c(Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1021/jm070024h
46882156 5677 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 404 7 4 4 3.3 CC(C)NC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078115 5677 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 404 7 4 4 3.3 CC(C)NC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
16113474 136608 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 455 8 4 5 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nncn1CCc1c[nH]c2ccccc12 10.1021/jm070024h
CHEMBL373993 136608 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 455 8 4 5 3.6 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nncn1CCc1c[nH]c2ccccc12 10.1021/jm070024h
59446105 172797 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)N(Cc1ccc(O)cc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
CHEMBL4514053 172797 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter methodDisplacement of [125I]-ghrelin (1 to 28 residues) from human GHS-R1a expressed in pig LLC-PK1 cell membranes by LKB gamma counter method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)N(Cc1ccc(O)cc1)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O nan
11556936 81582 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)N(Cc1ccc(O)cc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
CHEMBL2163472 81582 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 850 21 11 10 0.7 C[C@H](NC(=O)N(Cc1ccc(O)cc1)NC(=O)C(N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm300557t
60195114 81579 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 640 13 8 6 1.8 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm300557t
CHEMBL2163468 81579 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting methodDisplacement of [125I]ghrelin expressed in in LLC-PK1 cells incubated for 1 hr by gamma counting method
ChEMBL 640 13 8 6 1.8 CC(C)CN(NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/jm300557t
70690449 75842 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 486 9 0 5 4.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048810 75842 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 486 9 0 5 4.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
70692603 75848 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 463 7 0 5 5.0 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4nc5ccccc5s4)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048816 75848 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 463 7 0 5 5.0 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4nc5ccccc5s4)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
44389192 168622 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 471 4 1 4 6.2 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCCC1 10.1016/j.bmcl.2004.11.075
CHEMBL436275 168622 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 471 4 1 4 6.2 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1C(=O)N1CCCCCC1 10.1016/j.bmcl.2004.11.075
44394982 66108 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 523 9 1 6 5.7 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL184093 66108 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 523 9 1 6 5.7 CCN(CC)[C@H]1CC[C@H](NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)CC1 10.1016/j.bmcl.2004.06.060
CHEMBL335799 211541 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm0001727
CHEMBL61663 215816 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50Binding affinity towards human Growth hormone secretagogue receptor type 1 using competitive binding assay with radiolabeled [35S]-MK-0677 expressed as IC50
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CN)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/s0960-894x(01)00324-9
44445628 161875 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 541 10 2 6 5.5 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL415135 161875 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 541 10 2 6 5.5 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2cnccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
145950877 162971 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4175360 162971 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
11663710 124441 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 528 9 1 5 6.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
CHEMBL363995 124441 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)Ability to displace [125I]ghrelin from cloned human GHS-R expressed in CHO-K cells was determined (Kd of ghrelin is 0.4 nM)
ChEMBL 528 9 1 5 6.3 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCN2CCCCC2=O)cc1 10.1016/j.bmcl.2004.06.060
16113371 79124 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
CHEMBL2113318 79124 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human GHSR1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1016/j.bmcl.2007.10.113
16113371 79124 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1021/jm0704550
CHEMBL2113318 79124 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 587 11 4 6 5.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2)cc1 10.1021/jm0704550
11713497 123211 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 531 9 1 6 6.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)c(C)c1 10.1016/j.bmcl.2004.11.075
CHEMBL361349 123211 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 531 9 1 6 6.8 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2CCC2OCCCO2)c(C)c1 10.1016/j.bmcl.2004.11.075
122182045 121974 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 554 9 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCO5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
CHEMBL3593634 121974 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [125I]human ghrelin from rat ghrelin receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 554 9 2 7 4.6 CC(=O)N1C[C@@H]2C=C(c3cnc(NCc4ccc5c(c4)OCO5)c(C(=O)NCCOc4ccccc4)c3)C[C@H]1CC2 10.1016/j.bmc.2015.05.047
11646276 75905 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
CHEMBL205136 75905 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 364 6 3 7 3.4 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc([N+](=O)[O-])cc2)cc1 10.1021/jm0510934
122182046 121975 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 586 8 2 6 5.6 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCC3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593635 121975 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 586 8 2 6 5.6 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCC3)cc1Cl 10.1016/j.bmc.2015.05.047
44436828 91971 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 11 4 6 4.3 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL241664 91971 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 550 11 4 6 4.3 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3)=NNC2CCc2ccccc2)cc1 10.1021/jm0704550
CHEMBL410108 212776 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligandBinding affinity to cloned human growth hormone secretagogue receptor type 1 in a competitive binding assay with [35S]MK-0677 as a radiolabeled ligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O)C(C)C 10.1021/jm0001727
11538533 74972 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL203280 74972 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(NCc2ccc(S(C)(=O)=O)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL500468 214092 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligandBinding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1021/jm020985q
11538534 74985 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
CHEMBL203373 74985 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]ghrelin from human GHS receptor expressed in CHOK cellsDisplacement of [125I]ghrelin from human GHS receptor expressed in CHOK cells
ChEMBL 397 6 3 7 2.9 CCc1nc(N)nc(N)c1-c1ccc(CNc2ccc(S(C)(=O)=O)cc2)cc1 10.1021/jm0510934
122182047 121976 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
CHEMBL3593636 121976 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assayInverse agonist activity rat ghrelin receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 588 8 2 7 5.4 COc1ccc(CNC(=O)c2cc(C3=C[C@@H]4CC[C@H](C3)N(C(C)=O)C4)cnc2NCc2ccc3c(c2)OCO3)cc1Cl 10.1016/j.bmc.2015.05.047
70686293 75854 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 472 5 0 7 3.8 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-c5ncccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048822 75854 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPADisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA
ChEMBL 472 5 0 7 3.8 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-c5ncccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
122180016 121551 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 540 9 2 9 5.1 CCCn1cc(-c2cnc(NCc3ccc4ncsc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
CHEMBL3586022 121551 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assayInverse agonist activity at rat ghrelin receptor expressed in HEK293 cells by NFAT-RE-luciferase reporter gene assay
ChEMBL 540 9 2 9 5.1 CCCn1cc(-c2cnc(NCc3ccc4ncsc4c3)c(C(=O)NCC3COc4ccccc4O3)c2)cn1 10.1016/j.bmcl.2015.04.040
44389216 123828 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 442 6 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C#N)c1 10.1016/j.bmcl.2004.11.075
CHEMBL362595 123828 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 442 6 1 5 5.9 CCN(CC)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)c(C#N)c1 10.1016/j.bmcl.2004.11.075
44389248 122142 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 433 7 2 5 5.0 CCN(CCO)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
CHEMBL359714 122142 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 433 7 2 5 5.0 CCN(CCO)c1ccc(NC(=O)c2c(-c3c(Cl)cccc3Cl)noc2C)cc1 10.1016/j.bmcl.2004.11.075
145958774 162242 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
CHEMBL4163811 162242 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1 10.1021/acs.jmedchem.8b00322
44445609 97010 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 579 10 3 5 6.4 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
CHEMBL266961 97010 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cellsDisplacement of 125I]-His9-ghrelin from human GHSR1a expressed in LLCPK1 cells
ChEMBL 579 10 3 5 6.4 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@H](NC(=O)Cc2ccccn2)c2c[nH]c3ccccc23)cc1 10.1021/jm701292s
16114532 84667 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccccc1Cn1c(CCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
CHEMBL222610 84667 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I-His9]ghrelin from human GHS1a receptor expressed in LLC PK1 cells
ChEMBL 575 11 4 6 5.2 COc1ccccc1Cn1c(CCc2c[nH]c3ccccc23)nnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N 10.1021/jm070024h
23648250 79134 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 585 10 4 5 6.0 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
CHEMBL2113327 79134 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cellsDisplacement of [125I]His9-ghrelin from human cloned GHS1a receptor expressed in LLC PK1 cells
ChEMBL 585 10 4 5 6.0 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1 10.1021/jm0704550
44409764 77120 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 488 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
CHEMBL207792 77120 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human GHS receptor by binding assayInhibition of human GHS receptor by binding assay
ChEMBL 488 9 4 8 3.6 CS(=O)(=O)c1ccc(CNc2ccc(-c3c(N)nc(N)nc3CNCc3ccccc3)cc2)cc1 10.1016/j.bmcl.2006.01.012
44378979 12812 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 506 9 2 5 4.6 NCCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL1188586 12812 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 506 9 2 5 4.6 NCCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
CHEMBL536779 12812 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity for human growth hormone GH secretagogue (hGHsr) receptorBinding affinity for human growth hormone GH secretagogue (hGHsr) receptor
ChEMBL 506 9 2 5 4.6 NCCCCCCNC(=O)Cn1c(-c2ccc3ccccc3c2)nc2ccc(Br)cc2c1=O 10.1016/s0960-894x(99)00584-3
11197 1061 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 10.1016/j.bmcl.2020.126953
154699458 1061 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 10.1016/j.bmcl.2020.126953
CHEMBL4632411 1061 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter methodDisplacement of [125I]-ghrelin from human GHS-R1a stably expressed in HEK cell membrane measured after 60 mins by gamma counter method
ChEMBL 572 7 2 9 3.9 CCOc1cc(Cl)c(cc1N1CCOCC1)C(=O)NC(=O)Nc1nc2c(s1)cc(cc2)CN1CCN(CC1)C 10.1016/j.bmcl.2020.126953
CHEMBL498956 214065 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [35S]MK-0677 from human growth hormone secretagogue receptorDisplacement of [35S]MK-0677 from human growth hormone secretagogue receptor
ChEMBL None None None CCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O)C(C)C 10.1021/jm8014519
46882198 5728 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 460 12 4 4 4.9 CCCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL1078497 5728 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human GHS-R1aInhibition of human GHS-R1a
ChEMBL 460 12 4 4 4.9 CCCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC(C)(C)N)cc2)cc1 10.1016/j.bmcl.2009.08.076
CHEMBL3578017 211745 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
CHEMBL3578017 211745 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assayDisplacement of [125I]ghrelin from human eYFP-fused ghrelin receptor expressed in COS7 cells after 75 mins by competitive receptor binding assay
ChEMBL None None None CC(=O)NC(CNC(=O)CCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm501702q
145953855 162491 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
CHEMBL4167669 162491 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assayDisplacement of human [125I]-ghrelin from GHS-R1a (unknown origin) expressed in HEK293 cell membranes after 1 hr by radioligand binding assay
ChEMBL 426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1 10.1021/acs.jmedchem.8b00322
90666035 109291 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 437 6 0 8 2.8 COc1cccc(-n2cc3nc(C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
CHEMBL3218908 109291 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysisDisplacement of [125I]-ghrelin from GSH-R1a (unknown origin) overexpressed in HEK cells after 60 mins by gamma counting analysis
ChEMBL 437 6 0 8 2.8 COc1cccc(-n2cc3nc(C)n(C[C@H]4CCCN(C[C@H]5CCCO5)C4)c(=O)c3n2)c1 10.1039/C2MD20340E
328912 62546 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 505 5 1 4 7.0 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1CC1c2ccccc2CCN1C 10.1016/j.bmcl.2004.11.075
CHEMBL178266 62546 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of binding to human growth hormone secretagogue receptorInhibition of binding to human growth hormone secretagogue receptor
ChEMBL 505 5 1 4 7.0 Cc1onc(-c2c(Cl)cccc2Cl)c1C(=O)Nc1ccccc1CC1c2ccccc2CCN1C 10.1016/j.bmcl.2004.11.075
178024 1958 33 None - 1 Human 9.9 pKd = 9.9 Binding
Compound was evaluated for binding affinity using [35S]MK-0677 (800-1100 Ci/mmol), as radioligand having specific high activityCompound was evaluated for binding affinity using [35S]MK-0677 (800-1100 Ci/mmol), as radioligand having specific high activity
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm970342o
5867 1958 33 None - 1 Human 9.9 pKd = 9.9 Binding
Compound was evaluated for binding affinity using [35S]MK-0677 (800-1100 Ci/mmol), as radioligand having specific high activityCompound was evaluated for binding affinity using [35S]MK-0677 (800-1100 Ci/mmol), as radioligand having specific high activity
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm970342o
CHEMBL13817 1958 33 None - 1 Human 9.9 pKd = 9.9 Binding
Compound was evaluated for binding affinity using [35S]MK-0677 (800-1100 Ci/mmol), as radioligand having specific high activityCompound was evaluated for binding affinity using [35S]MK-0677 (800-1100 Ci/mmol), as radioligand having specific high activity
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm970342o
57398340 71247 0 None - 1 Human 11.0 pKi = 11 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 449 5 0 8 4.6 Cc1nc2ccc(Oc3ccc4ncsc4c3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956993 71247 0 None - 1 Human 11.0 pKi = 11 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 449 5 0 8 4.6 Cc1nc2ccc(Oc3ccc4ncsc4c3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57400002 71248 0 None - 1 Human 11.0 pKi = 11 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 488 5 0 6 4.9 Cc1nc2ccc(Oc3ccc(Br)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956994 71248 0 None - 1 Human 11.0 pKi = 11 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 488 5 0 6 4.9 Cc1nc2ccc(Oc3ccc(Br)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57394881 71264 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 489 5 0 7 4.3 Cc1nc2ncc(Oc3ccc(Br)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957010 71264 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 489 5 0 7 4.3 Cc1nc2ncc(Oc3ccc(Br)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57393073 71255 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 449 5 0 8 4.6 Cc1nc2cnc(Oc3ccc4ncsc4c3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957001 71255 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 449 5 0 8 4.6 Cc1nc2cnc(Oc3ccc4ncsc4c3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
56926461 69007 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923609 69007 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
56926462 69008 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923610 69008 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
56926680 69021 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccccc2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923623 69021 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccccc2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
56926682 69023 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923625 69023 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
11664206 69024 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923626 69024 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
56926893 69034 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 nan
CHEMBL1923637 69034 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 nan
11526745 69039 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL1923642 69039 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134137202 142801 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 5 3 6 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3893048 142801 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 552 5 3 6 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(OC)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134137257 143112 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 540 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3895776 143112 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 540 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
134133352 143480 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3898794 143480 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2Cl)NC(=O)[C@@H](C)N(C)C1=O nan
11527086 144025 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 574 3 3 5 3.4 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)c(Cl)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3903118 144025 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 574 3 3 5 3.4 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)c(Cl)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
11512561 144344 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 574 3 3 5 3.4 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2Cl)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3905791 144344 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 574 3 3 5 3.4 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2Cl)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134133037 144542 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3907497 144542 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H](C)N(C)C1=O nan
134132670 144589 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3907891 144589 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134132152 144907 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3910300 144907 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 572 4 3 5 3.9 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@@H](C)N(C)C1=O nan
134142839 145361 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3913855 145361 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 5 2.8 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134142553 145422 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3914259 145422 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134143635 145549 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2Cl)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3915269 145549 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2Cl)NC(=O)C2(CCCC2)NC1=O nan
134143096 145908 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 584 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2ccc(Br)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3918009 145908 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 584 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2ccc(Br)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134142204 145912 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3918046 145912 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 4 4 5 4.0 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
11584702 146166 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 540 3 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3920049 146166 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 540 3 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134139279 146422 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 594 4 4 5 4.1 CCC(C)[C@H]1NCCOc2ccccc2[C@H]2C[C@@H]2CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3922056 146422 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 594 4 4 5 4.1 CCC(C)[C@H]1NCCOc2ccccc2[C@H]2C[C@@H]2CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134138445 147352 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NC/C=C/c2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3929593 147352 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NC/C=C/c2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134138218 147985 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NC/C=C\c2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3934367 147985 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 538 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NC/C=C\c2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134148686 148147 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3935670 148147 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134149719 148663 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 2 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C(C)(C)C)C(=O)N1C nan
CHEMBL3939872 148663 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 2 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C(C)(C)C)C(=O)N1C nan
134145791 148762 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2c(F)c(F)c(F)c(F)c2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3940705 148762 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 3 3 5 2.8 C[C@@H]1C(=O)N[C@H](Cc2c(F)c(F)c(F)c(F)c2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134143746 150576 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 2 4 5 3.9 O=C1NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1cccc(Cl)c1 nan
CHEMBL3955179 150576 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 578 2 4 5 3.9 O=C1NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1cccc(Cl)c1 nan
134145221 150608 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CCC(C)C1NC[C@H](C)Oc2ccccc2CCCNC(=O)C(Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3955437 150608 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CCC(C)C1NC[C@H](C)Oc2ccccc2CCCNC(=O)C(Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134155656 151170 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3959816 151170 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2cccc(Cl)c2)NC(=O)[C@@H](C)N(C)C1=O nan
134155282 151318 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3961108 151318 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134153496 152261 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 3 5 2.4 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL3969367 152261 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 3 5 2.4 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O nan
134153654 152742 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 632 3 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(I)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3973513 152742 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 632 3 3 5 2.7 C[C@@H]1C(=O)N[C@H](Cc2ccc(I)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
134157569 154012 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 560 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2cc(F)c(F)c(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3984338 154012 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 560 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2cc(F)c(F)c(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C nan
57345600 71244 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 488 5 0 6 4.9 Cc1nc2ncc(Oc3ccc(Br)cc3F)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956990 71244 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 488 5 0 6 4.9 Cc1nc2ncc(Oc3ccc(Br)cc3F)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57345599 71245 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 444 5 0 6 4.8 Cc1nc2ccc(Oc3ccc(Cl)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956991 71245 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 444 5 0 6 4.8 Cc1nc2ccc(Oc3ccc(Cl)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57398341 71253 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 444 5 0 6 4.8 Cc1nc2cnc(Oc3ccc(Cl)cc3F)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956999 71253 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 444 5 0 6 4.8 Cc1nc2cnc(Oc3ccc(Cl)cc3F)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
178024 1958 33 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm960054c
5867 1958 33 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm960054c
CHEMBL13817 1958 33 None - 1 Human 9.6 pKi = 9.6 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10.1021/jm960054c
57398342 71261 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 450 5 0 9 4.0 Cc1nc2ncc(Oc3ccc4ncsc4c3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957007 71261 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 450 5 0 9 4.0 Cc1nc2ncc(Oc3ccc4ncsc4c3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57401803 71263 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 469 6 0 7 5.1 Cc1nc2ncc(Oc3ccc(-c4ccccc4)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957009 71263 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 469 6 0 7 5.1 Cc1nc2ncc(Oc3ccc(-c4ccccc4)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57401799 71254 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 436 5 0 8 3.7 Cc1nc2cnc(Oc3ccc4c(c3)OCO4)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957000 71254 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 436 5 0 8 3.7 Cc1nc2cnc(Oc3ccc4c(c3)OCO4)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57399248 69015 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
CHEMBL1923617 69015 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O nan
44340008 113361 0 None - 1 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 583 9 2 6 3.2 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)c(F)c1)C(=O)N1CCC2=NN(C(C)(C)C)C(=O)C2(Cc2ccccc2)C1 10.1016/s0960-894x(02)00734-5
CHEMBL331801 113361 0 None - 1 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 583 9 2 6 3.2 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)c(F)c1)C(=O)N1CCC2=NN(C(C)(C)C)C(=O)C2(Cc2ccccc2)C1 10.1016/s0960-894x(02)00734-5
57399248 69015 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923617 69015 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 556 4 3 5 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
24970113 69027 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 580 3 3 5 3.8 C[C@@H]1CN[C@@H](C2CCCCC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923629 69027 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 580 3 3 5 3.8 C[C@@H]1CN[C@@H](C2CCCCC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
57391293 71251 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 468 6 0 6 5.7 Cc1nc2ccc(Oc3ccc(-c4ccccc4)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956997 71251 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 468 6 0 6 5.7 Cc1nc2ccc(Oc3ccc(-c4ccccc4)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
162659411 181201 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 575 13 3 7 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CC#N)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4761419 181201 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 575 13 3 7 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CC#N)cc1 10.1021/acs.jmedchem.9b02122
44340268 110494 0 None - 1 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 609 10 2 6 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)c(F)c1)C(=O)N1CCC2=NN(CC(F)(F)F)C(=O)C2(Cc2ccccc2)C1 10.1016/s0960-894x(02)00734-5
CHEMBL325062 110494 0 None - 1 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 609 10 2 6 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)c(F)c1)C(=O)N1CCC2=NN(CC(F)(F)F)C(=O)C2(Cc2ccccc2)C1 10.1016/s0960-894x(02)00734-5
57401800 71257 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 446 5 0 8 3.9 Cc1nc2cnc(Oc3ccc4c(c3)ncn4C)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957003 71257 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 446 5 0 8 3.9 Cc1nc2cnc(Oc3ccc4c(c3)ncn4C)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
162657606 181093 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 693 15 3 8 5.7 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4760409 181093 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 693 15 3 8 5.7 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
57401801 71259 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 445 5 0 7 4.2 Cc1nc2ncc(Oc3ccc(Cl)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957005 71259 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 445 5 0 7 4.2 Cc1nc2ncc(Oc3ccc(Cl)cc3F)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
162672839 182998 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 681 14 3 7 5.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4793824 182998 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 681 14 3 7 5.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL500468 214092 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)CNC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)O 10.1021/jm300414b
56942242 125169 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645257 125169 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 566 12 4 7 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CO)cc1 10.1016/j.bmcl.2016.04.003
56925343 69037 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 550 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cccc3c2O[C@H](CC3)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923640 69037 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 550 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cccc3c2O[C@H](CC3)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
57398339 71246 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 436 5 0 8 3.7 Cc1nc2ccc(Oc3ccc4c(c3)OCO4)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956992 71246 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 436 5 0 8 3.7 Cc1nc2ccc(Oc3ccc4c(c3)OCO4)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
162645413 179702 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 677 14 3 7 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4744051 179702 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 677 14 3 7 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(C)cc2)cc1 10.1021/acs.jmedchem.9b02122
155540883 172933 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4517399 172933 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
16133832 213308 18 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/acs.jmedchem.8b01644
CHEMBL425281 213308 18 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL None None None CCCCCCCC(=O)OC[C@H](NC(=O)[C@H](CO)NC(=O)CN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C 10.1021/acs.jmedchem.8b01644
162653781 180458 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 732 15 4 8 6.2 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3c[nH]c4ccccc34)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4753046 180458 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 732 15 4 8 6.2 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3c[nH]c4ccccc34)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
57401802 71260 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 437 5 0 9 3.1 Cc1nc2ncc(Oc3ccc4c(c3)OCO4)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957006 71260 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 437 5 0 9 3.1 Cc1nc2ncc(Oc3ccc4c(c3)OCO4)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57401797 71240 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 468 6 0 6 5.7 Cc1nc2ncc(Oc3ccc(-c4ccccc4)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956987 71240 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 468 6 0 6 5.7 Cc1nc2ncc(Oc3ccc(-c4ccccc4)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
57398343 71262 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 462 5 0 8 4.1 Cc1nc2ncc(Oc3ccc(F)c4cccnc34)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957008 71262 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 462 5 0 8 4.1 Cc1nc2ncc(Oc3ccc(F)c4cccnc34)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
56926175 68984 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 68984 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69006 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69006 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69014 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69014 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69022 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69022 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69032 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69032 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69033 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69033 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69035 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69035 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69040 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69040 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142348 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142348 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142371 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142371 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142443 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142443 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142482 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142482 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142518 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142518 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142577 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142577 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142851 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142851 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142874 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142874 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143211 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143211 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143326 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143326 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143327 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143327 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143428 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143428 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143669 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143669 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143986 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143986 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144636 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144636 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144788 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144788 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144838 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144838 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144839 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144839 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145135 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145135 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145159 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145159 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145262 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145262 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145301 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145301 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145350 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145350 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145735 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145735 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145833 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145833 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146037 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146037 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146348 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146348 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146379 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146379 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146529 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146529 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146628 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146628 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146704 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146704 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146765 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146765 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146969 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146969 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147093 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147093 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147388 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147388 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147727 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147727 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147730 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147730 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147990 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147990 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148330 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148330 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148429 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148429 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148450 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148450 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148496 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148496 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148519 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148519 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148756 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148756 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148995 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148995 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149066 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149066 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149080 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149080 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149102 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149102 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149425 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149425 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149465 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149465 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149739 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149739 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149761 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149761 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150067 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150067 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150126 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150126 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150250 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150250 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150262 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150262 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150307 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150307 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150311 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150311 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150988 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150988 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150990 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150990 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151068 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151068 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151355 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151355 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151622 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151622 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152091 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152091 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152132 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152132 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152275 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152275 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152418 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152418 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152508 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152508 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152696 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152696 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152875 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152875 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153037 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153037 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153080 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153080 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153144 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153144 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153295 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153295 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153435 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153435 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153499 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153499 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153648 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153648 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153834 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153834 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153933 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153933 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154030 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154030 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154238 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154238 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154276 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154276 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 125167 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645255 125167 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
162646324 179712 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 688 17 3 9 4.8 CCN(CC)CCc1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(OC)cc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4744139 179712 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 688 17 3 9 4.8 CCN(CC)CCc1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(OC)cc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
162665018 182111 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 550 12 3 6 4.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(C)=O)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4782214 182111 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 550 12 3 6 4.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(C)=O)cc1 10.1021/acs.jmedchem.9b02122
58438451 92256 0 None 2089 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 442 4 0 6 3.1 Cc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426689 92256 0 None 2089 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 442 4 0 6 3.1 Cc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
90644553 111708 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 540 5 1 7 4.0 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN([C@@H]3CCc5cc(-c6ccc(C(N)=O)nc6)ccc53)C4)nc2s1 10.1021/ml400473x
CHEMBL3287214 111708 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 540 5 1 7 4.0 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN([C@@H]3CCc5cc(-c6ccc(C(N)=O)nc6)ccc53)C4)nc2s1 10.1021/ml400473x
56926177 68986 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 68986 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 68988 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 68988 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 68989 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 68989 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 68990 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 68990 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69011 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69011 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69028 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69028 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69030 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69030 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69031 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 69031 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 83500 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 83500 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142370 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142370 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142610 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142610 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142695 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142695 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142729 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142729 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142894 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 142894 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143316 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143316 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143494 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143494 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143643 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143643 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143652 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143652 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143706 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143706 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143969 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 143969 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144054 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144054 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144090 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144090 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144113 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144113 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144307 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144307 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144367 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144367 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144460 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144460 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144486 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144486 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144540 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144540 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144624 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144624 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144676 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144676 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144903 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144903 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144946 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 144946 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145113 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145113 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145185 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145185 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145318 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145318 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145377 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145377 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145435 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145435 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145448 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145448 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145711 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145711 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145909 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 145909 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146314 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146314 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146595 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146595 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146640 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146640 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146670 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 146670 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147200 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147200 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147362 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147362 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147529 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147529 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147611 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147611 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147640 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147640 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147949 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147949 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147961 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 147961 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148052 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148052 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148110 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148110 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148141 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148141 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148294 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148294 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148341 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148341 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148455 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148455 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148581 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148581 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148675 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148675 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148778 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148778 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148999 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 148999 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149002 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149002 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149006 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149006 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149010 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149010 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149091 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149091 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149289 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149289 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149411 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149411 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149422 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149422 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149674 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149674 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149793 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149793 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149833 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149833 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149914 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149914 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149942 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 149942 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150088 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150088 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150117 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150117 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150133 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150133 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150428 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150428 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150465 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150465 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150503 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150503 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150633 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 150633 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151013 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151013 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151026 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151026 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151327 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151327 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151378 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151378 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151386 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151386 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151524 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151524 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151581 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151581 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151799 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151799 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151802 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151802 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151832 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151832 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151901 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 151901 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152055 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152055 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152346 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152346 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152370 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152370 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152378 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152378 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152379 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152379 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152424 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152424 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152487 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152487 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152555 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152555 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152720 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152720 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152801 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 152801 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153184 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153184 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153188 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153188 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153194 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153194 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153330 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153330 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153356 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153356 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153378 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153378 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153459 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153459 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153542 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153542 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153607 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153607 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153627 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153627 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153724 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153724 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153737 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 153737 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154128 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154128 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154322 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 154322 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence 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 68985 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 3 5 2.1 CCC[C@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL1923505 68985 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 3 5 2.1 CCC[C@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
56926266 68987 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 523 6 4 6 1.4 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CCCCN)C1=O nan
CHEMBL1923508 68987 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 523 6 4 6 1.4 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CCCCN)C1=O nan
134133634 143609 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 549 4 4 6 2.7 CC(C)C[C@@H]1NCCOc2cccnc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3899825 143609 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 549 4 4 6 2.7 CC(C)C[C@@H]1NCCOc2cccnc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
57722117 143659 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 466 2 3 5 1.3 C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3900193 143659 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 466 2 3 5 1.3 C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
57722068 143908 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 478 3 3 6 0.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCOCCOCCN[C@@H](C2CC2)C(=O)N1C nan
CHEMBL3902231 143908 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 478 3 3 6 0.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCOCCOCCN[C@@H](C2CC2)C(=O)N1C nan
134135595 143939 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 598 4 4 5 5.1 CC(C)C[C@@H]1NCc2ccccc2Sc2ccccc2CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3902597 143939 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 598 4 4 5 5.1 CC(C)C[C@@H]1NCc2ccccc2Sc2ccccc2CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
134139160 146184 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 560 4 3 5 3.7 CC(C)C[C@H]1C(=O)NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN1C nan
CHEMBL3920156 146184 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 560 4 3 5 3.7 CC(C)C[C@H]1C(=O)NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN1C nan
134140250 146221 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 562 5 4 5 3.7 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](CCc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3920479 146221 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 562 5 4 5 3.7 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](CCc2ccccc2)NC(=O)C2(CCCC2)NC1=O nan
57951693 146252 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.4 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O nan
CHEMBL3920711 146252 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.4 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O nan
134140177 146345 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CC(C)C[C@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3921493 146345 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 5 4.3 CC(C)C[C@H]1NC[C@H](C)Oc2ccccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134139639 146614 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 6 4 7 2.5 CCOC(=O)CC[C@@H]1NC(=O)C2(CCCC2)NC(=O)[C@H](CC(C)C)NCCOc2ccccc2/C=C\CNC1=O nan
CHEMBL3923467 146614 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 556 6 4 7 2.5 CCOC(=O)CC[C@@H]1NC(=O)C2(CCCC2)NC(=O)[C@H](CC(C)C)NCCOc2ccccc2/C=C\CNC1=O nan
134140216 146619 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 587 4 5 5 3.8 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3923508 146619 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 587 4 5 5 3.8 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)C2(CCCC2)NC1=O nan
134141155 146703 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 6 3.3 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCOC2)NC1=O nan
CHEMBL3924187 146703 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 596 4 4 6 3.3 CC[C@H](C)[C@@H]1NC[C@H](C)Oc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCOC2)NC1=O nan
134137626 147458 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 4 5 6 3.0 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3930400 147458 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 4 5 6 3.0 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)C2(CCCC2)NC1=O nan
134148332 148257 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 583 4 4 6 3.3 CC[C@H](C)[C@@H]1NCCOc2ncccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3936664 148257 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 583 4 4 6 3.3 CC[C@H](C)[C@@H]1NCCOc2ncccc2CCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
57528213 148460 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 3 5 2.9 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O nan
CHEMBL3938163 148460 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 3 5 2.9 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]2CCCN2C1=O nan
134149424 148612 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 3 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](C(C)c2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3939431 148612 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 3 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](C(C)c2ccccc2)NC(=O)CN(C)C1=O nan
57951672 149570 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.4 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
CHEMBL3946954 149570 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.4 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
134147008 149912 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 4 4 5 2.8 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C(C)(C)NC1=O nan
CHEMBL3949653 149912 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 522 4 4 5 2.8 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C(C)(C)NC1=O nan
134155726 150994 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 478 3 3 6 0.2 CC1C(=O)NC(Cc2ccc(F)cc2)C(=O)NCCOCCOCCNC(C2CC2)C(=O)N1C nan
CHEMBL3958492 150994 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 478 3 3 6 0.2 CC1C(=O)NC(Cc2ccc(F)cc2)C(=O)NCCOCCOCCNC(C2CC2)C(=O)N1C nan
134155844 151064 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 570 6 4 5 3.3 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC1=O nan
CHEMBL3959055 151064 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 570 6 4 5 3.3 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC1=O nan
57528307 151103 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O nan
CHEMBL3959346 151103 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 520 4 3 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O nan
134156186 151326 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 490 4 4 4 3.1 CC[C@H](C)[C@@H]1NCCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3961157 151326 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 490 4 4 4 3.1 CC[C@H](C)[C@@H]1NCCCCCNC(=O)[C@H](Cc2cccc(Cl)c2)NC(=O)C2(CCCC2)NC1=O nan
134150525 151540 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 551 8 5 6 2.2 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O nan
CHEMBL3963236 151540 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 551 8 5 6 2.2 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O nan
134149894 151810 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.2 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccc(Cl)cc1 nan
CHEMBL3965402 151810 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 614 4 4 5 4.2 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1ccc(Cl)cc1 nan
134150119 152023 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 6 4 6 3.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](COC(C)(C)C)NC1=O nan
CHEMBL3967266 152023 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 580 6 4 6 3.2 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](COC(C)(C)C)NC1=O nan
134150914 152056 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 6 3 5 3.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]([C@H](C)CC)N(C)C1=O nan
CHEMBL3967522 152056 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 564 6 3 5 3.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]([C@H](C)CC)N(C)C1=O nan
57722047 152843 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 436 4 3 4 1.8 CCC[C@@H]1NCc2cccc(c2)CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3974323 152843 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 436 4 3 4 1.8 CCC[C@@H]1NCc2cccc(c2)CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
57951687 152848 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 4 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O nan
CHEMBL3974356 152848 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 4 4 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)NC1=O nan
57528291 152892 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 3 5 2.9 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O nan
CHEMBL3974776 152892 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 3 5 2.9 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C1=O nan
134152485 153152 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 604 5 4 6 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(C(=O)O)cc2)NC(=O)C2(CCCC2)N(C)C1=O nan
CHEMBL3976941 153152 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 604 5 4 6 3.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccc(C(=O)O)cc2)NC(=O)C2(CCCC2)N(C)C1=O nan
134151873 153176 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 630 4 4 5 4.7 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1cccc2ccccc12 nan
CHEMBL3977166 153176 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 630 4 4 5 4.7 O=C1NC2(CCCC2)C(=O)N[C@@H](Cc2ccccc2)C(=O)NC/C=C\c2ccccc2OCCN[C@H]1Cc1cccc2ccccc12 nan
76556607 153531 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 2 5 2.8 CCC(C)C1NCCOc2ccccc2CCCNC(=O)C(Cc2ccccc2)N2CCC(C2=O)N(C)C1=O nan
CHEMBL3980176 153531 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 534 4 2 5 2.8 CCC(C)C1NCCOc2ccccc2CCCNC(=O)C(Cc2ccccc2)N2CCC(C2=O)N(C)C1=O nan
134157812 153646 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 4 5 2.1 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O nan
CHEMBL3981235 153646 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 506 3 4 5 2.1 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O nan
134156737 153675 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 547 4 4 6 2.8 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccncc2)NC(=O)C2(CCCC2)NC1=O nan
CHEMBL3981446 153675 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 547 4 4 6 2.8 CC(C)C[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccncc2)NC(=O)C2(CCCC2)NC1=O nan
134156806 154070 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 6 4 5 3.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(C)C)NC1=O nan
CHEMBL3984892 154070 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 536 6 4 5 3.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(C)C)NC1=O nan
134157124 154182 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 492 2 4 5 1.9 O=C1CNCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)N1 nan
CHEMBL3985913 154182 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 492 2 4 5 1.9 O=C1CNCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)N1 nan
11706547 69017 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 540 3 3 5 2.8 CC(C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923619 69017 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 540 3 3 5 2.8 CC(C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
134138625 148006 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 3 3 5 1.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3934561 148006 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 494 3 3 5 1.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
44434011 147839 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 465 12 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL393321 147839 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 465 12 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCc1ccccc1 10.1016/j.bmcl.2007.07.099
70692601 75846 0 None - 1 Human 8.0 pKi = 8.0 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 481 7 0 7 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048814 75846 0 None - 1 Human 8.0 pKi = 8.0 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 481 7 0 7 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
127046957 139682 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 649 12 3 7 5.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc(F)cc(F)n2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798155 139682 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 649 12 3 7 5.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2cc(F)cc(F)n2)cc1 10.1016/j.bmcl.2016.04.003
127046472 139669 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798056 139669 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
56926266 68987 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 523 6 4 6 1.4 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CCCCN)C1=O 10.1021/jm2007062
CHEMBL1923508 68987 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 523 6 4 6 1.4 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](CCCCN)C1=O 10.1021/jm2007062
73352329 92236 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 6 0 6 3.8 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H](C)c2ccc(-c4ncccn4)cc2)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426669 92236 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 6 0 6 3.8 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H](C)c2ccc(-c4ncccn4)cc2)C3)nc1 10.1016/j.bmcl.2013.07.044
70692602 75847 0 None - 1 Human 6.9 pKi = 6.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 423 8 0 5 3.5 CCCOc1ccc(CN2CC3(CCN(C(=O)Cc4ccc(OC)cc4)CC3)C2)cn1 10.1016/j.bmcl.2012.05.024
CHEMBL2048815 75847 0 None - 1 Human 6.9 pKi = 6.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 423 8 0 5 3.5 CCCOc1ccc(CN2CC3(CCN(C(=O)Cc4ccc(OC)cc4)CC3)C2)cn1 10.1016/j.bmcl.2012.05.024
162665974 182211 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 612 13 3 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4783347 182211 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 612 13 3 6 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
44396381 67501 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 558 13 2 3 6.2 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NCc1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm040103i
CHEMBL189625 67501 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 558 13 2 3 6.2 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NCc1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm040103i
44396377 66913 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 532 13 2 4 5.8 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(Cc1ccc(C)o1)C(=O)NC1CCCCC1 10.1021/jm040103i
CHEMBL186647 66913 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 532 13 2 4 5.8 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(Cc1ccc(C)o1)C(=O)NC1CCCCC1 10.1021/jm040103i
44396269 67326 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 426 10 2 3 4.2 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C)C(=O)NC(C)(C)C 10.1021/jm040103i
CHEMBL188586 67326 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 426 10 2 3 4.2 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C)C(=O)NC(C)(C)C 10.1021/jm040103i
56926895 69036 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 552 3 3 5 3.0 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OC(C)(C)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923639 69036 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 552 3 3 5 3.0 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OC(C)(C)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
56942244 125171 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645259 125171 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 632 12 5 7 4.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
162648546 179854 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 536 13 3 6 3.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC=O)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4745666 179854 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 536 13 3 6 3.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC=O)cc1 10.1021/acs.jmedchem.9b02122
58438460 111711 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL3287217 111711 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml400473x
56926356 68990 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923512 68990 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
56926176 68985 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 3 5 2.1 CCC[C@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923505 68985 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 3 5 2.1 CCC[C@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
71453390 81814 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 526 6 2 4 4.4 C=CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164500 81814 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 526 6 2 4 4.4 C=CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
162663952 182128 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 636 13 2 7 6.6 COc1ccc(/C=C(\C#N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4782383 182128 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 636 13 2 7 6.6 COc1ccc(/C=C(\C#N)C(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
118725963 117168 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 541 7 1 7 3.6 COc1ccc(OCC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
CHEMBL3394203 117168 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 541 7 1 7 3.6 COc1ccc(OCC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
44434112 168836 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2cc3ccccc3n2S(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL438154 168836 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2cc3ccccc3n2S(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
3174463 66738 4 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 532 12 2 3 6.2 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(F)cc1 10.1021/jm040103i
CHEMBL185876 66738 4 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 532 12 2 3 6.2 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(F)cc1 10.1021/jm040103i
56926464 69010 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)N(C)C1=O nan
CHEMBL1923612 69010 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)N(C)C1=O nan
118725960 117164 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 507 5 0 6 4.5 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C#N)c1 10.1021/ml500414n
CHEMBL3394199 117164 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 507 5 0 6 4.5 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C#N)c1 10.1021/ml500414n
162657547 180959 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 694 15 2 9 6.2 COc1ccc(/C=C(\C#N)C(=O)OCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4758721 180959 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 694 15 2 9 6.2 COc1ccc(/C=C(\C#N)C(=O)OCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
162658148 181124 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 565 13 4 7 3.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CN)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4760746 181124 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 565 13 4 7 3.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CN)cc1 10.1021/acs.jmedchem.9b02122
162662164 181386 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 636 12 3 6 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C#Cc2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4763700 181386 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 636 12 3 6 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C#Cc2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
127047362 139694 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 590 11 5 7 4.7 COc1ccc(Cn2c([C@H](N)Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798204 139694 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 590 11 5 7 4.7 COc1ccc(Cn2c([C@H](N)Cc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
3154000 124244 4 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 530 12 3 4 5.8 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(O)cc1 10.1021/jm040103i
CHEMBL363467 124244 4 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 530 12 3 4 5.8 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(O)cc1 10.1021/jm040103i
162651277 180172 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 598 14 3 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNCc2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4749525 180172 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 598 14 3 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNCc2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
3180629 67323 5 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 518 11 2 3 5.8 CCN(CC)CCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(F)cc1 10.1021/jm040103i
CHEMBL188582 67323 5 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 518 11 2 3 5.8 CCN(CC)CCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(F)cc1 10.1021/jm040103i
44434016 90164 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 415 12 3 7 1.5 CCCCNC(=O)CCn1nnnc1[C@@H](CCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL238228 90164 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 415 12 3 7 1.5 CCCCNC(=O)CCn1nnnc1[C@@H](CCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
72190452 92249 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 474 5 0 6 4.4 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H]2CCc4cc(-c5nccs5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426682 92249 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 474 5 0 6 4.4 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H]2CCc4cc(-c5nccs5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
118725964 117169 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 539 7 1 6 4.1 COc1ccc(CCC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
CHEMBL3394204 117169 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 539 7 1 6 4.1 COc1ccc(CCC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
70692600 75845 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 447 7 0 7 2.8 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048813 75845 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 447 7 0 7 2.8 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4nccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
70682036 75849 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 446 7 1 4 4.3 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4n[nH]c5ccccc45)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048817 75849 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 446 7 1 4 4.3 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4n[nH]c5ccccc45)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
70686293 75854 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 472 5 0 7 3.8 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-c5ncccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048822 75854 0 None - 1 Human 7.9 pKi = 7.9 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 472 5 0 7 3.8 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-c5ncccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
58438460 111711 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml500414n
CHEMBL3287217 111711 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml500414n
162660604 181195 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 700 15 3 9 5.0 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCN3CCCCC3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4761319 181195 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 700 15 3 9 5.0 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCN3CCCCC3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
162671996 182807 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 707 16 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)NCCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4791255 182807 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 707 16 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)NCCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
25032438 116170 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human ghrelin receptor by receptor binding assayBinding affinity to human ghrelin receptor by receptor binding assay
ChEMBL 485 14 2 6 3.8 CCN(CC)CCCS(=O)(=O)N[C@H](CCc1ccccc1)c1nc(-c2ccc(OC)cc2)n[nH]1 10.1021/jm5003183
CHEMBL3358450 116170 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human ghrelin receptor by receptor binding assayBinding affinity to human ghrelin receptor by receptor binding assay
ChEMBL 485 14 2 6 3.8 CCN(CC)CCCS(=O)(=O)N[C@H](CCc1ccccc1)c1nc(-c2ccc(OC)cc2)n[nH]1 10.1021/jm5003183
11692516 69019 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 554 3 3 5 3.1 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923621 69019 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 554 3 3 5 3.1 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
67407161 92255 0 None 1819 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 467 5 0 5 4.3 CCc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426688 92255 0 None 1819 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 467 5 0 5 4.3 CCc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
67410074 111710 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccc(C)n5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL3287216 111710 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccc(C)n5)ccc42)C3)nc1 10.1021/ml400473x
56926782 69028 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 472 4 3 4 3.0 CC[C@H](C)[C@@H]1NCCCCCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923631 69028 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 472 4 3 4 3.0 CC[C@H](C)[C@@H]1NCCCCCCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
70696687 75844 0 None - 1 Human 6.8 pKi = 6.8 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 446 7 0 6 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4cccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048812 75844 0 None - 1 Human 6.8 pKi = 6.8 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 446 7 0 6 3.4 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-n4cccn4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
127046806 139908 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 638 13 4 7 5.4 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799604 139908 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 638 13 4 7 5.4 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
127048038 139947 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 551 11 4 7 4.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799862 139947 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 551 11 4 7 4.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
44434076 89748 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 513 10 2 9 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC1CN(S(C)(=O)=O)c2ccccc21 10.1016/j.bmcl.2007.07.099
CHEMBL237717 89748 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 513 10 2 9 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC1CN(S(C)(=O)=O)c2ccccc21 10.1016/j.bmcl.2007.07.099
56926463 69009 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923611 69009 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
11526696 71573 17 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923502 71573 17 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1963249 71573 17 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
72191051 92233 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 456 5 0 6 3.4 CCc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426666 92233 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 456 5 0 6 3.4 CCc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
58438460 111711 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL3287217 111711 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml400473x
56926783 69029 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 470 4 3 4 2.8 CC[C@H](C)[C@@H]1NCCCC/C=C/CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923632 69029 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 470 4 3 4 2.8 CC[C@H](C)[C@@H]1NCCCC/C=C/CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
162658631 181059 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 561 12 3 7 3.6 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C#N)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4759983 181059 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 561 12 3 7 3.6 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C#N)cc1 10.1021/acs.jmedchem.9b02122
118725958 117163 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 507 4 0 7 3.9 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)Cc4nn(C)c5ncccc45)CC3)C2)ncn1 10.1021/ml500414n
CHEMBL3394197 117163 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 507 4 0 7 3.9 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)Cc4nn(C)c5ncccc45)CC3)C2)ncn1 10.1021/ml500414n
162659337 181292 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 665 15 3 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C(C#N)Cc2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4762631 181292 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 665 15 3 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C(C#N)Cc2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
73355325 92238 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 6 0 6 3.8 COc1ccc(CC(=O)N2CCC3(CC2)CN(C(C)c2ccc(-c4ncccn4)cc2)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426671 92238 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 6 0 6 3.8 COc1ccc(CC(=O)N2CCC3(CC2)CN(C(C)c2ccc(-c4ncccn4)cc2)C3)nc1 10.1016/j.bmcl.2013.07.044
70696688 75850 0 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 487 9 0 6 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cn1 10.1016/j.bmcl.2012.05.024
CHEMBL2048818 75850 0 None - 1 Human 7.8 pKi = 7.8 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 487 9 0 6 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cn1 10.1016/j.bmcl.2012.05.024
127048060 139836 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 789 20 6 10 5.4 COC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799222 139836 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 789 20 6 10 5.4 COC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
56942388 139918 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799687 139918 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 613 12 3 7 5.3 COc1ccc(Cn2c([C@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
162677361 183485 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 685 16 4 8 4.7 COc1ccc(C[C@@H](N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4799766 183485 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 685 16 4 8 4.7 COc1ccc(C[C@@H](N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
58438475 92244 0 None 1548 2 Human 7.8 pKi = 7.8 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml400473x
CHEMBL2426677 92244 0 None 1548 2 Human 7.8 pKi = 7.8 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml400473x
44434109 146256 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 529 13 2 9 1.8 CN(c1ccccc1CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N)S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL392076 146256 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 529 13 2 9 1.8 CN(c1ccccc1CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N)S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
134139080 147658 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
CHEMBL3931856 147658 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 4 4 5 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O nan
44434010 88744 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 445 14 3 8 1.5 CCCCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL236311 88744 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 445 14 3 8 1.5 CCCCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
127047655 139589 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797531 139589 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
44340007 9282 0 None - 1 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 541 9 2 6 2.0 CN1N=C2CCN(C(=O)[C@@H](COCc3ccc(F)c(F)c3)NC(=O)C(C)(C)N)CC2(Cc2ccccc2)C1=O 10.1016/s0960-894x(02)00734-5
CHEMBL111026 9282 0 None - 1 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 541 9 2 6 2.0 CN1N=C2CCN(C(=O)[C@@H](COCc3ccc(F)c(F)c3)NC(=O)C(C)(C)N)CC2(Cc2ccccc2)C1=O 10.1016/s0960-894x(02)00734-5
56925344 69038 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 550 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cccc3c2O[C@@H](CC3)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923641 69038 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 550 3 3 5 2.5 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cccc3c2O[C@@H](CC3)CN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
44434083 90002 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 420 10 2 7 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C/C=C/c1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL238155 90002 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 420 10 2 7 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C/C=C/c1ccccc1 10.1016/j.bmcl.2007.07.099
44434050 145425 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL391428 145425 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1 10.1016/j.bmcl.2007.07.099
44396306 67247 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 452 11 2 3 4.7 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C)C(=O)NC1CCCCC1 10.1021/jm040103i
CHEMBL188173 67247 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 452 11 2 3 4.7 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C)C(=O)NC1CCCCC1 10.1021/jm040103i
145948725 167473 0 None - 1 Human 8.7 pKi = 8.7 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 885 20 7 9 6.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL4299615 167473 0 None - 1 Human 8.7 pKi = 8.7 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 885 20 7 9 6.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
57345597 71241 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 410 5 0 6 4.2 Cc1nc2ccc(Oc3ccc(F)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956988 71241 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 410 5 0 6 4.2 Cc1nc2ccc(Oc3ccc(F)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
56942243 125170 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645258 125170 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 621 12 4 8 3.6 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CNCCO2)cc1 10.1016/j.bmcl.2016.04.003
162648837 179814 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 706 15 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4745116 179814 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 706 15 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
127048059 139541 0 None - 1 Human 8.6 pKi = 8.6 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 675 16 6 8 4.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797225 139541 0 None - 1 Human 8.6 pKi = 8.6 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 675 16 6 8 4.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
11526745 69039 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923642 69039 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
57400003 71250 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 461 5 0 7 4.7 Cc1nc2ccc(Oc3ccc(F)c4cccnc34)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956996 71250 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 461 5 0 7 4.7 Cc1nc2ccc(Oc3ccc(F)c4cccnc34)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
155529391 171416 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1427 41 20 17 -3.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4463042 171416 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1427 41 20 17 -3.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
70690449 75842 0 None - 1 Human 7.7 pKi = 7.7 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 486 9 0 5 4.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048810 75842 0 None - 1 Human 7.7 pKi = 7.7 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 486 9 0 5 4.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(OCC(C)C)cc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
118725965 117170 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 539 6 1 6 4.0 CNC(=O)c1cc(OC)ccc1CC(=O)N1CCC2(CC1)CN([C@@H]1CCc3cc(-c4cc(C)ncn4)ccc31)C2 10.1021/ml500414n
CHEMBL3394205 117170 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 539 6 1 6 4.0 CNC(=O)c1cc(OC)ccc1CC(=O)N1CCC2(CC1)CN([C@@H]1CCc3cc(-c4cc(C)ncn4)ccc31)C2 10.1021/ml500414n
44434080 89882 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL237933 89882 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1 10.1016/j.bmcl.2007.07.099
162647450 179847 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 536 12 2 6 4.6 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN(C)C)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4745548 179847 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 536 12 2 6 4.6 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN(C)C)cc1 10.1021/acs.jmedchem.9b02122
71456910 81872 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 480 5 2 4 3.6 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164823 81872 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 480 5 2 4 3.6 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
3154005 66743 5 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 550 13 1 4 5.7 CCN(CC)CCCN(C(=O)CCN1CCCc2ccccc21)C(C(=O)NC1CCCCC1)c1ccc(F)cc1 10.1021/jm040103i
CHEMBL185887 66743 5 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 550 13 1 4 5.7 CCN(CC)CCCN(C(=O)CCN1CCCc2ccccc21)C(C(=O)NC1CCCCC1)c1ccc(F)cc1 10.1021/jm040103i
70696689 75853 0 None - 1 Human 6.7 pKi = 6.7 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 460 5 0 7 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5cccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048821 75853 0 None - 1 Human 6.7 pKi = 6.7 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 460 5 0 7 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5cccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
56926681 69022 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2cccc(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923624 69022 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2cccc(F)c2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
127047409 139606 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 888 24 8 10 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C(CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797639 139606 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 888 24 8 10 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C(CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
56926785 69031 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923634 69031 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 508 4 3 5 2.3 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
70688404 75838 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1021/ml400473x
CHEMBL2048807 75838 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1021/ml400473x
44434009 167429 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 431 13 3 8 1.1 CCCCNC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL429799 167429 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 431 13 3 8 1.1 CCCCNC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
53248756 61151 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I]Ghrelin binding to human Ghrelin receptor expressed in CHO-K1 cells after 60 mins by liquid scintillation spectrometryInhibition of [125I]Ghrelin binding to human Ghrelin receptor expressed in CHO-K1 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 457 5 0 5 5.6 Cc1ccccc1-c1nc2ccc(Oc3ccc(F)cc3)cc2c(=O)n1C[C@H]1CCCN(C)C1 10.1016/j.bmc.2011.02.021
CHEMBL1765654 61151 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I]Ghrelin binding to human Ghrelin receptor expressed in CHO-K1 cells after 60 mins by liquid scintillation spectrometryInhibition of [125I]Ghrelin binding to human Ghrelin receptor expressed in CHO-K1 cells after 60 mins by liquid scintillation spectrometry
ChEMBL 457 5 0 5 5.6 Cc1ccccc1-c1nc2ccc(Oc3ccc(F)cc3)cc2c(=O)n1C[C@H]1CCCN(C)C1 10.1016/j.bmc.2011.02.021
CHEMBL2170701 209338 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cn(C)c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
10253999 123767 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 466 12 2 3 5.1 CCC(C(=O)NC1CCCCC1)N(CCCN(CC)CC)C(=O)c1ccc(-c2ccccc2)[nH]1 10.1021/jm040103i
CHEMBL362303 123767 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 466 12 2 3 5.1 CCC(C(=O)NC1CCCCC1)N(CCCN(CC)CC)C(=O)c1ccc(-c2ccccc2)[nH]1 10.1021/jm040103i
127048061 139711 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 903 24 7 11 5.9 COC(=O)[C@H](CC(C)C)NC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798337 139711 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 903 24 7 11 5.9 COC(=O)[C@H](CC(C)C)NC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1 10.1016/j.bmcl.2016.04.003
162662593 181946 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 591 12 3 7 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN2CCC(N)CC2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4780100 181946 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 591 12 3 7 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN2CCC(N)CC2)cc1 10.1021/acs.jmedchem.9b02122
44579909 186879 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL489819 186879 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
44434073 89571 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL237507 89571 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
70694649 75855 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 475 5 0 7 3.2 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-n3nccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
CHEMBL2048823 75855 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 475 5 0 7 3.2 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-n3nccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
162659161 181367 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 642 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)Cc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4763471 181367 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 642 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)Cc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
162652815 180352 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 564 14 2 6 5.3 CCN(CC)CC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4751674 180352 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 564 14 2 6 5.3 CCN(CC)CC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL2170779 209343 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44434008 146509 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 404 11 2 9 0.7 COC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL392268 146509 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 404 11 2 9 0.7 COC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
44434110 88483 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 515 13 3 9 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL235135 88483 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 515 13 3 9 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
44577060 188028 0 None -69 8 Human 6.6 pKi = 6.6 Binding
Inhibition of ghrelin receptorInhibition of ghrelin receptor
ChEMBL 530 10 1 4 4.8 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL497746 188028 0 None -69 8 Human 6.6 pKi = 6.6 Binding
Inhibition of ghrelin receptorInhibition of ghrelin receptor
ChEMBL 530 10 1 4 4.8 CC(C)[C@H](NC(=O)CCN(C)C)c1cccc(F)c1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1016/j.bmc.2008.03.072
CHEMBL2170780 209344 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
71453404 81874 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)N[C@]2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164826 81874 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)N[C@]2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(Cl)cc32)CC1 10.1016/j.bmc.2012.07.018
70692603 75848 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 463 7 0 5 5.0 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4nc5ccccc5s4)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048816 75848 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 463 7 0 5 5.0 CC(C)COc1ccc(CN2CC3(CCN(C(=O)Cc4nc5ccccc5s4)CC3)C2)cc1 10.1016/j.bmcl.2012.05.024
56926360 69006 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 522 4 3 5 2.7 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923608 69006 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 522 4 3 5 2.7 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
72190451 92247 0 None 524 2 Human 7.6 pKi = 7.6 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL2426680 92247 0 None 524 2 Human 7.6 pKi = 7.6 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1021/ml400473x
44579907 187024 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)[C@H](C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL491044 187024 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)[C@H](C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
73350846 92237 0 None -1 2 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 6 0 6 3.8 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H](C)c2ccc(-c4ncccn4)cc2)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426670 92237 0 None -1 2 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 6 0 6 3.8 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H](C)c2ccc(-c4ncccn4)cc2)C3)nc1 10.1016/j.bmcl.2013.07.044
44576247 214199 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity at GHS-R1a (unknown origin) assessed as inhibition constantBinding affinity at GHS-R1a (unknown origin) assessed as inhibition constant
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.1c02191
CHEMBL506986 214199 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity at GHS-R1a (unknown origin) assessed as inhibition constantBinding affinity at GHS-R1a (unknown origin) assessed as inhibition constant
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.1c02191
44576247 214199 0 None - 1 Human 6.6 pKi = 6.6 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1016/j.bmcl.2016.04.003
CHEMBL506986 214199 0 None - 1 Human 6.6 pKi = 6.6 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1016/j.bmcl.2016.04.003
44579880 186811 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
CHEMBL489401 186811 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2008.07.120
118725962 117167 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 526 6 1 7 3.1 COc1cc(C(N)=O)c(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccc(C)n5)ccc42)C3)cn1 10.1021/ml500414n
CHEMBL3394202 117167 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 526 6 1 7 3.1 COc1cc(C(N)=O)c(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccc(C)n5)ccc42)C3)cn1 10.1021/ml500414n
44396384 67378 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 574 14 2 5 6.1 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(OC)c(OC)c1 10.1021/jm040103i
CHEMBL188839 67378 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 574 14 2 5 6.1 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccc(OC)c(OC)c1 10.1021/jm040103i
44434074 154649 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
CHEMBL399625 154649 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 501 12 3 9 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2ccccc2NS(C)(=O)=O)n1 10.1016/j.bmcl.2007.07.099
70684155 75856 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 486 5 0 6 4.1 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-c3ncccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
CHEMBL2048824 75856 0 None - 1 Human 7.6 pKi = 7.6 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 486 5 0 6 4.1 O=C(Cc1cn2cc(Cl)ccc2n1)N1CCC2(CC1)CN(Cc1ccc(-c3ncccn3)cc1)C2 10.1016/j.bmcl.2012.05.024
72191050 92234 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 453 4 0 5 4.0 Cc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426667 92234 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 453 4 0 5 4.0 Cc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
72190449 92243 0 None 4 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426676 92243 0 None 4 2 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
118725966 117171 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 539 6 1 6 4.6 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(NC(C)=O)c1 10.1021/ml500414n
CHEMBL3394206 117171 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 539 6 1 6 4.6 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(NC(C)=O)c1 10.1021/ml500414n
162675268 183334 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 645 13 3 8 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C2(C#N)CCOCC2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4797685 183334 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 645 13 3 8 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C2(C#N)CCOCC2)cc1 10.1021/acs.jmedchem.9b02122
3153999 126805 3 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 494 14 2 3 5.9 CCCCC(C(=O)NC1CCCCC1)N(CCCN(CC)CC)C(=O)c1ccc(-c2ccccc2)[nH]1 10.1021/jm040103i
CHEMBL365489 126805 3 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 494 14 2 3 5.9 CCCCC(C(=O)NC1CCCCC1)N(CCCN(CC)CC)C(=O)c1ccc(-c2ccccc2)[nH]1 10.1021/jm040103i
71451551 81822 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 460 5 2 4 3.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(C)cc32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164508 81822 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 460 5 2 4 3.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)c(C)cc32)CC1 10.1016/j.bmc.2012.07.018
72190451 92247 0 None 524 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426680 92247 0 None 524 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
72190451 92247 0 None 524 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL2426680 92247 0 None 524 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)nc1 10.1021/ml400473x
9950632 88677 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2007.07.099
CHEMBL236038 88677 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N 10.1016/j.bmcl.2007.07.099
127046472 139669 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at GHS-R1a (unknown origin) assessed as inhibition constantBinding affinity at GHS-R1a (unknown origin) assessed as inhibition constant
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1021/acs.jmedchem.1c02191
CHEMBL3798056 139669 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at GHS-R1a (unknown origin) assessed as inhibition constantBinding affinity at GHS-R1a (unknown origin) assessed as inhibition constant
ChEMBL 902 24 8 10 5.6 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](N)CCCCN)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1021/acs.jmedchem.1c02191
127045859 139674 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at GHS-R1a (unknown origin) assessed as inhibition constantBinding affinity at GHS-R1a (unknown origin) assessed as inhibition constant
ChEMBL 831 20 7 9 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CO)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1021/acs.jmedchem.1c02191
CHEMBL3798095 139674 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at GHS-R1a (unknown origin) assessed as inhibition constantBinding affinity at GHS-R1a (unknown origin) assessed as inhibition constant
ChEMBL 831 20 7 9 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CO)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1021/acs.jmedchem.1c02191
127045859 139674 0 None - 1 Human 8.5 pKi = 8.5 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 831 20 7 9 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CO)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798095 139674 0 None - 1 Human 8.5 pKi = 8.5 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 831 20 7 9 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CO)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
127047523 140038 0 None - 1 Human 8.5 pKi = 8.5 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 859 20 7 9 6.0 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3800422 140038 0 None - 1 Human 8.5 pKi = 8.5 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 859 20 7 9 6.0 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)O)cc1 10.1016/j.bmcl.2016.04.003
71456897 81821 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 513 5 2 3 5.7 CCN1CCC(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164507 81821 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 513 5 2 3 5.7 CCN1CCC(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
162653916 180521 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 707 15 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4753794 180521 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 707 15 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1 10.1021/acs.jmedchem.9b02122
162643920 181756 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 679 14 4 8 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4777792 181756 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 679 14 4 8 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
155537651 172292 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1597 47 22 19 -3.8 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(N)=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4475293 172292 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1597 47 22 19 -3.8 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(N)=O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
57391292 71249 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 473 6 0 8 4.6 COc1ccc2cccc(Oc3ccc4nc(C)n(C[C@H]5CCCN(C(C)C)C5)c(=O)c4n3)c2n1 10.1016/j.bmcl.2012.01.078
CHEMBL1956995 71249 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 473 6 0 8 4.6 COc1ccc2cccc(Oc3ccc4nc(C)n(C[C@H]5CCCN(C(C)C)C5)c(=O)c4n3)c2n1 10.1016/j.bmcl.2012.01.078
57345598 71258 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 411 5 0 7 3.5 Cc1nc2ncc(Oc3ccc(F)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957004 71258 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 411 5 0 7 3.5 Cc1nc2ncc(Oc3ccc(F)cc3)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
53373577 92253 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 458 5 0 7 2.8 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426686 92253 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 458 5 0 7 2.8 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
57391294 71252 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 410 5 0 6 4.2 Cc1nc2cnc(Oc3ccc(F)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956998 71252 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 410 5 0 6 4.2 Cc1nc2cnc(Oc3ccc(F)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
155526063 171012 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1174 34 16 14 -2.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4456830 171012 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1174 34 16 14 -2.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
162663004 182025 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 603 13 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C(C)(C)C#N)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4781141 182025 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 603 13 3 7 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C(C)(C)C#N)cc1 10.1021/acs.jmedchem.9b02122
155557019 174563 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4556887 174563 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
71453489 209345 15 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.8b01644
CHEMBL2170781 209345 15 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/acs.jmedchem.8b01644
67405379 92250 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 474 5 0 6 4.4 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccs5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426683 92250 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 474 5 0 6 4.4 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccs5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
25211977 186878 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 372 7 1 3 3.9 C[C@H](Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL489818 186878 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 372 7 1 3 3.9 C[C@H](Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
25098836 191434 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL519322 191434 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@H](C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
127047525 139742 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 858 20 7 9 5.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798559 139742 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 858 20 7 9 5.9 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
162653309 180449 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 718 14 5 8 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4752936 180449 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 718 14 5 8 5.9 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
44579756 186799 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
CHEMBL489370 186799 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 372 7 1 3 3.9 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1 10.1016/j.bmcl.2008.07.120
162666964 182486 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 536 13 3 6 4.6 CCNCC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4787023 182486 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 536 13 3 6 4.6 CCNCC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL2170693 209330 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1csc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
44434121 89879 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 385 11 2 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCC#N 10.1016/j.bmcl.2007.07.099
CHEMBL237927 89879 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 385 11 2 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCC#N 10.1016/j.bmcl.2007.07.099
56926584 69018 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 554 4 3 5 3.2 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923620 69018 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 554 4 3 5 3.2 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
44434120 89878 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 523 15 3 9 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCCNC(=O)OCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL237926 89878 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 523 15 3 9 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCCNC(=O)OCc1ccccc1 10.1016/j.bmcl.2007.07.099
44434007 88546 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 390 10 2 9 0.3 COC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL235446 88546 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 390 10 2 9 0.3 COC(=O)CCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
11541143 69016 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 540 4 3 5 3.0 CCC[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923618 69016 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 540 4 3 5 3.0 CCC[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
24969520 69020 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 520 3 3 5 2.5 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923622 69020 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 520 3 3 5 2.5 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL2170694 209331 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
56926580 69012 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 536 5 4 5 3.1 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CC)NC1=O 10.1021/jm2007062
CHEMBL1923614 69012 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 536 5 4 5 3.1 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CC)NC1=O 10.1021/jm2007062
162653802 180507 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 656 15 4 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CCc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4753592 180507 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 656 15 4 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CCc2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
73346226 92235 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 487 8 0 7 3.4 COCC(c1ccc(-c2ncccn2)cc1)N1CC2(CCN(C(=O)Cc3ccc(OC)cn3)CC2)C1 10.1016/j.bmcl.2013.07.044
CHEMBL2426668 92235 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 487 8 0 7 3.4 COCC(c1ccc(-c2ncccn2)cc1)N1CC2(CCN(C(=O)Cc3ccc(OC)cn3)CC2)C1 10.1016/j.bmcl.2013.07.044
162674738 183363 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 638 14 3 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4797988 183363 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 638 14 3 6 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
56926177 68986 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923506 68986 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
56926581 69013 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 550 5 4 5 3.4 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C(C)C)NC1=O 10.1021/jm2007062
CHEMBL1923615 69013 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 550 5 4 5 3.4 CC[C@H](C)[C@@H]1NC[C@@H](C)Oc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C(C)C)NC1=O 10.1021/jm2007062
71458747 81809 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2012.07.018
CHEMBL2164494 81809 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 446 4 2 4 2.9 Cc1cc2c(cc1Cl)NC(=O)C2(NC(=O)CN1CCN(C)CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2012.07.018
23631116 4081 23 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 409 5 0 5 4.8 Fc1ccc(cc1)Oc1ccc2c(c1)c(=O)n(c(n2)C)C[C@H]1CCCN(C1)C(C)C 10.1016/j.bmcl.2012.01.078
3538 4081 23 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 409 5 0 5 4.8 Fc1ccc(cc1)Oc1ccc2c(c1)c(=O)n(c(n2)C)C[C@H]1CCCN(C1)C(C)C 10.1016/j.bmcl.2012.01.078
CHEMBL243001 4081 23 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 409 5 0 5 4.8 Fc1ccc(cc1)Oc1ccc2c(c1)c(=O)n(c(n2)C)C[C@H]1CCCN(C1)C(C)C 10.1016/j.bmcl.2012.01.078
127046956 139932 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 631 12 3 7 5.5 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799776 139932 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 631 12 3 7 5.5 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ncccc2F)cc1 10.1016/j.bmcl.2016.04.003
118725961 117165 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 523 6 0 7 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C#N)c1 10.1021/ml500414n
CHEMBL3394200 117165 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 523 6 0 7 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C#N)c1 10.1021/ml500414n
162663407 182006 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 562 13 3 6 4.3 C=CC(=O)NCC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4780843 182006 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 562 13 3 6 4.3 C=CC(=O)NCC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
56926462 69008 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923610 69008 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
70695747 73162 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Ghrelin from human GHSR1a receptorDisplacement of [125I]Ghrelin from human GHSR1a receptor
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
CHEMBL2011816 73162 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Ghrelin from human GHSR1a receptorDisplacement of [125I]Ghrelin from human GHSR1a receptor
ChEMBL 540 8 2 5 4.7 CC(C)[C@H](C(=O)NC1CCN(Cc2ccccc2)CC1)N1CC(=O)Nc2ccc(Oc3ccccc3)cc2C1=O 10.1016/j.bmcl.2012.01.014
67406334 111707 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 498 4 0 7 4.3 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN([C@@H]3CCc5cc(-c6ncccn6)ccc53)C4)nc2s1 10.1021/ml400473x
CHEMBL3287213 111707 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 498 4 0 7 4.3 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN([C@@H]3CCc5cc(-c6ncccn6)ccc53)C4)nc2s1 10.1021/ml400473x
57390496 69026 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
CHEMBL1923628 69026 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
71453489 209345 15 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
CHEMBL2170781 209345 15 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assayDisplacement of [125I]-His-ghrelin from human ghrelin receptor expressed in COS7 cells incubated for 75 mins by scintillation counting based assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O 10.1021/jm300414b
56926269 68989 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 460 5 3 5 2.0 CCCC[C@H]1NC(=O)CN(C)C(=O)[C@H](CCC)NCCOc2ccccc2CCCNC1=O 10.1021/jm2007062
CHEMBL1923511 68989 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 460 5 3 5 2.0 CCCC[C@H]1NC(=O)CN(C)C(=O)[C@H](CCC)NCCOc2ccccc2CCCNC1=O 10.1021/jm2007062
56926784 69030 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 506 4 3 4 2.9 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923633 69030 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 506 4 3 4 2.9 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
70688404 75838 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1021/ml400473x
CHEMBL2048807 75838 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1021/ml400473x
70688404 75838 0 None - 1 Human 6.4 pKi = 6.4 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048807 75838 0 None - 1 Human 6.4 pKi = 6.4 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 464 6 0 5 4.3 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc4c(c2)CCC(C)(C)O4)C3)cc1 10.1016/j.bmcl.2012.05.024
44434123 145525 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 343 8 2 8 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC#N 10.1016/j.bmcl.2007.07.099
CHEMBL391510 145525 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 343 8 2 8 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC#N 10.1016/j.bmcl.2007.07.099
56926582 69014 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](CCc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923616 69014 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 536 5 3 5 3.1 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](CCc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
16114404 154873 24 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 508 11 3 6 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL400814 154873 24 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 508 11 3 6 4.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN)cc1 10.1021/acs.jmedchem.9b02122
25190383 81880 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164831 81880 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 466 4 2 4 3.2 CN1CCN(CC(=O)NC2(c3ccc(Cl)cc3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
11683187 199909 44 None -457 5 Human 5.4 pKi = 5.4 Binding
Binding affinity to ghrelin receptorBinding affinity to ghrelin receptor
ChEMBL 419 7 0 8 2.9 COCc1nnc(N2CC(Oc3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1016/j.bmcl.2009.11.097
CHEMBL594828 199909 44 None -457 5 Human 5.4 pKi = 5.4 Binding
Binding affinity to ghrelin receptorBinding affinity to ghrelin receptor
ChEMBL 419 7 0 8 2.9 COCc1nnc(N2CC(Oc3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1016/j.bmcl.2009.11.097
70684154 75840 0 None - 1 Human 6.4 pKi = 6.4 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 414 6 0 4 3.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccccc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048809 75840 0 None - 1 Human 6.4 pKi = 6.4 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 414 6 0 4 3.9 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccccc2Cl)C3)cc1 10.1016/j.bmcl.2012.05.024
44434055 89276 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL236858 89276 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccccc1NS(C)(=O)=O 10.1016/j.bmcl.2007.07.099
56942385 125172 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645260 125172 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 618 13 5 7 4.5 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
56942535 139736 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 593 12 4 7 4.4 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798525 139736 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 593 12 4 7 4.4 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
24180592 96984 0 None -134 6 Human 6.3 pKi = 6.3 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
CHEMBL266647 96984 0 None -134 6 Human 6.3 pKi = 6.3 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 560 11 1 4 5.7 CC(C)C[C@H](NC(=O)CCN(C)C)c1cc(Cl)ccc1N1CCN(C(=O)[C@H](C)Cc2ccc(Cl)cc2)CC1 10.1021/jm701137s
44434113 88620 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 452 10 2 9 1.5 COC(=O)C(c1ccccc1)n1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
CHEMBL235793 88620 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 452 10 2 9 1.5 COC(=O)C(c1ccccc1)n1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N 10.1016/j.bmcl.2007.07.099
44434051 89386 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccccc2)n1 10.1016/j.bmcl.2007.07.099
CHEMBL237058 89386 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccccc2)n1 10.1016/j.bmcl.2007.07.099
118725954 117161 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 467 4 0 5 4.3 Cc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml500414n
CHEMBL3394193 117161 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 467 4 0 5 4.3 Cc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)nc1 10.1021/ml500414n
24969603 69025 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 520 3 3 5 2.4 Cc1ccc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NCCOc3ccccc3CCCNC2=O)cc1 10.1021/jm2007062
CHEMBL1923627 69025 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 520 3 3 5 2.4 Cc1ccc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NCCOc3ccccc3CCCNC2=O)cc1 10.1021/jm2007062
57394882 71265 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 447 5 0 9 3.3 Cc1nc2ncc(Oc3ccc4c(c3)ncn4C)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957011 71265 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 447 5 0 9 3.3 Cc1nc2ncc(Oc3ccc4c(c3)ncn4C)nc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
9876514 9108 2 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 610 10 2 7 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)cc1F)C(=O)N1CCC2=NN(CC(F)(F)F)C(=O)[C@]2(Cc2ccccn2)C1 10.1016/s0960-894x(02)00734-5
CHEMBL109980 9108 2 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 610 10 2 7 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)cc1F)C(=O)N1CCC2=NN(CC(F)(F)F)C(=O)[C@]2(Cc2ccccn2)C1 10.1016/s0960-894x(02)00734-5
70682037 75852 20 None 43 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 495 5 0 8 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1 10.1016/j.bmcl.2013.07.044
CHEMBL2048820 75852 20 None 43 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 495 5 0 8 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1 10.1016/j.bmcl.2013.07.044
145948708 167472 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 886 20 7 10 5.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CNCCO3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL4299606 167472 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 886 20 7 10 5.2 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CNCCO3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(C)=O)cc1 10.1016/j.bmcl.2016.04.003
67410074 111710 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccc(C)n5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL3287216 111710 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5nccc(C)n5)ccc42)C3)nc1 10.1021/ml400473x
56926465 69011 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 4 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O 10.1021/jm2007062
CHEMBL1923613 69011 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 4 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O 10.1021/jm2007062
44434119 89877 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 400 10 3 10 -0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1nnn[nH]1 10.1016/j.bmcl.2007.07.099
CHEMBL237925 89877 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 400 10 3 10 -0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1nnn[nH]1 10.1016/j.bmcl.2007.07.099
70694648 75843 0 None - 1 Human 7.3 pKi = 7.3 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 462 7 0 7 3.6 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-c4nnc(C)o4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
CHEMBL2048811 75843 0 None - 1 Human 7.3 pKi = 7.3 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 462 7 0 7 3.6 COc1ccc(OCC(=O)N2CCC3(CC2)CN(Cc2ccc(-c4nnc(C)o4)cc2)C3)cc1 10.1016/j.bmcl.2012.05.024
155561671 175640 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 817 22 11 9 -0.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4581511 175640 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 817 22 11 9 -0.5 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
56926894 69035 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
CHEMBL1923638 69035 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 C[C@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2O1 10.1021/jm2007062
162672372 183062 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 656 14 3 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C=C/c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4794448 183062 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 656 14 3 6 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C=C/c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.9b02122
56925345 69040 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(F)ccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923643 69040 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 542 3 3 5 2.3 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2cc(F)ccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
56926464 69010 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923612 69010 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)N(C)C1=O 10.1021/jm2007062
56942387 139637 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 579 13 4 7 4.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3797857 139637 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 579 13 4 7 4.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL105462 208445 38 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL None None None C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm960054c
56926680 69021 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccccc2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923623 69021 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccccc2F)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
162649014 179917 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 702 14 4 7 6.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2c[nH]c3ccccc23)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4746362 179917 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 702 14 4 7 6.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2c[nH]c3ccccc23)cc1 10.1021/acs.jmedchem.9b02122
162666112 182290 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 638 13 3 8 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)c2ccc(C#N)nc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4784240 182290 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 638 13 3 8 4.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)c2ccc(C#N)nc2)cc1 10.1021/acs.jmedchem.9b02122
162676229 183280 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 715 15 3 10 3.9 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4797064 183280 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 715 15 3 10 3.9 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(N(C)C)cc2)cc1 10.1021/acs.jmedchem.9b02122
58438475 92244 0 None 1548 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426677 92244 0 None 1548 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
58438475 92244 0 None 1548 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml400473x
CHEMBL2426677 92244 0 None 1548 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml400473x
56926461 69007 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923609 69007 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 522 4 3 5 2.7 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
118725956 117162 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 493 5 0 5 4.9 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)Cc4ccc(C5CC5)cn4)CC3)C2)ncn1 10.1021/ml500414n
CHEMBL3394195 117162 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 493 5 0 5 4.9 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)Cc4ccc(C5CC5)cn4)CC3)C2)ncn1 10.1021/ml500414n
155551597 173925 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 974 27 13 11 -1.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
CHEMBL4541252 173925 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL 974 27 13 11 -1.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(N)=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.8b01644
57394797 71256 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 461 5 0 7 4.7 Cc1nc2cnc(Oc3ccc(F)c4cccnc34)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1957002 71256 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 461 5 0 7 4.7 Cc1nc2cnc(Oc3ccc(F)c4cccnc34)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
162649450 180030 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 725 14 3 10 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C2CCN(c3oc(C)nc3C#N)CC2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4747770 180030 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 725 14 3 10 5.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)C2CCN(c3oc(C)nc3C#N)CC2)cc1 10.1021/acs.jmedchem.9b02122
58438464 3043 35 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
9060 3043 35 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
CHEMBL3287218 3043 35 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
DB14870 3043 35 None 1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
58438464 3043 35 None 1 3 Human 8.2 pKi = 8.2 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
9060 3043 35 None 1 3 Human 8.2 pKi = 8.2 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
CHEMBL3287218 3043 35 None 1 3 Human 8.2 pKi = 8.2 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
DB14870 3043 35 None 1 3 Human 8.2 pKi = 8.2 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 10.1021/ml400473x
67406334 111707 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 498 4 0 7 4.3 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN([C@@H]3CCc5cc(-c6ncccn6)ccc53)C4)nc2s1 10.1021/ml400473x
CHEMBL3287213 111707 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 498 4 0 7 4.3 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN([C@@H]3CCc5cc(-c6ncccn6)ccc53)C4)nc2s1 10.1021/ml400473x
57401798 71242 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 410 5 0 6 4.2 Cc1nc2ncc(Oc3ccc(F)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
CHEMBL1956989 71242 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation countingDisplacement of [125I]-Ghrelin from human GHSR membranes overexpressing GSH-R1a by scintillation counting
ChEMBL 410 5 0 6 4.2 Cc1nc2ncc(Oc3ccc(F)cc3)cc2c(=O)n1C[C@H]1CCCN(C(C)C)C1 10.1016/j.bmcl.2012.01.078
58438475 92244 0 None 1548 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml500414n
CHEMBL2426677 92244 0 None 1548 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 468 5 0 5 4.3 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncccn5)ccc42)C3)cc1 10.1021/ml500414n
11541319 69041 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 556 3 3 5 2.7 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2O1 10.1021/jm2007062
CHEMBL1923644 69041 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 556 3 3 5 2.7 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccc(F)cc2O1 10.1021/jm2007062
162659375 181327 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 566 14 4 7 3.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNCC(=O)O)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4763077 181327 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 566 14 4 7 3.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNCC(=O)O)cc1 10.1021/acs.jmedchem.9b02122
127046807 139915 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799671 139915 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
127047654 139952 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799883 139952 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 571 11 3 7 5.2 COc1ccc(Cn2c([C@@H](N)Cc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
121879 2222 24 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm960054c
5868 2222 24 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm960054c
CHEMBL308716 2222 24 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligandBinding Affinity against Growth hormone secretagogue receptor of swine using [35S]MK-0677 as radioligand
ChEMBL 509 7 3 6 3.6 O=C(CC(N)(C)C)N[C@@H]1CCc2c(N(C1=O)Cc1ccc(cc1)c1ccccc1c1nnn[nH]1)cccc2 10.1021/jm960054c
162665952 182355 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 688 14 4 10 3.5 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4785149 182355 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 688 14 4 10 3.5 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1 10.1021/acs.jmedchem.9b02122
134139753 146011 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 5 3 5 2.5 CCCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
CHEMBL3918783 146011 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting methodDisplacement of [125I]-Ghrelin from human GSHR1a transfected in HEK293 cell membranes after 30 mins by microplate scintillation and luminescence counting method
ChEMBL 508 5 3 5 2.5 CCCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O nan
162663868 181964 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 672 14 3 9 3.8 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4780408 181964 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 672 14 3 9 3.8 COc1ccc(Cn2c(CCN3CCOCC3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
56926268 68988 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 542 4 3 5 2.5 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](Cc2ccccc2)C1=O 10.1021/jm2007062
CHEMBL1923510 68988 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 542 4 3 5 2.5 CN1CC(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](Cc2ccccc2)C1=O 10.1021/jm2007062
56926175 68984 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923504 68984 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
23635235 166477 0 None -239 5 Human 6.2 pKi = 6.2 Binding
Inhibition of ghrelin receptorInhibition of ghrelin receptor
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmc.2008.03.072
CHEMBL427860 166477 0 None -239 5 Human 6.2 pKi = 6.2 Binding
Inhibition of ghrelin receptorInhibition of ghrelin receptor
ChEMBL 526 10 1 4 4.9 Cc1ccc(N2CCN(C(=O)[C@H](C)Cc3ccc(Cl)cc3)CC2)c([C@@H](NC(=O)CCN(C)C)C(C)C)c1 10.1016/j.bmc.2008.03.072
70686292 75851 0 None - 1 Human 7.2 pKi = 7.2 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 461 5 0 8 3.0 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048819 75851 0 None - 1 Human 7.2 pKi = 7.2 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 461 5 0 8 3.0 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3)C4)nc2s1 10.1016/j.bmcl.2012.05.024
90644554 111709 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ccncn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL3287215 111709 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 469 5 0 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ccncn5)ccc42)C3)nc1 10.1021/ml400473x
70682037 75852 20 None 43 2 Human 8.2 pKi = 8.2 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 495 5 0 8 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1 10.1016/j.bmcl.2012.05.024
CHEMBL2048820 75852 20 None 43 2 Human 8.2 pKi = 8.2 Binding
Antagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIAAntagonist activity at human GHS-R1a expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP binding by DELFIA
ChEMBL 495 5 0 8 3.6 Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1 10.1016/j.bmcl.2012.05.024
11664206 69024 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923626 69024 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 574 3 3 5 3.1 C[C@@H]1C(=O)N[C@H](Cc2ccc(C(F)(F)F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
216208 9695 33 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1016/s0960-894x(02)00734-5
CHEMBL113313 9695 33 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.In vitro binding affinity against human type 1a growth hormone secretagogue receptor (hGHS-R1a), using [125I]ghrelin as radioligand.
ChEMBL 505 9 2 6 1.7 CN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@@]2(Cc2ccccc2)C1=O 10.1016/s0960-894x(02)00734-5
56926682 69023 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
CHEMBL1923625 69023 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 524 3 3 5 2.2 C[C@@H]1C(=O)N[C@H](Cc2ccc(F)cc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C 10.1021/jm2007062
67408128 92251 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 5 0 6 3.4 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426684 92251 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 457 5 0 6 3.4 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-n5nccn5)ccc42)C3)cc1 10.1016/j.bmcl.2013.07.044
24180646 148158 0 None -1023 8 Human 6.1 pKi = 6.1 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1021/jm701137s
CHEMBL393576 148158 0 None -1023 8 Human 6.1 pKi = 6.1 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 591 11 2 5 4.7 CC(C)C[C@H](NCCN)c1cccc(F)c1N1CCN(C(=O)[C@@H](Cc2ccc(Cl)cc2Cl)N2CCCC2=O)CC1 10.1021/jm701137s
57390496 69026 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
CHEMBL1923628 69026 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 552 3 3 5 2.9 Cc1cc(C[C@H]2NC(=O)[C@@H](C)N(C)C(=O)[C@H](C3CC3)NC[C@@H](C)Oc3ccccc3CCCNC2=O)ccc1F 10.1021/jm2007062
CHEMBL501261 214112 23 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assayDisplacement of [125I]-His9 ghrelin from SNAP-tagged human GHSR expressed in HEK293T cells after 3 hrs by HTRF assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.8b01644
56926892 69033 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923636 69033 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 534 4 3 4 3.7 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
44434012 89045 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 479 13 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL236513 89045 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 479 13 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCc1ccccc1 10.1016/j.bmcl.2007.07.099
127046473 139755 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 661 17 6 8 4.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3798645 139755 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assayCompetitive binding affinity to human SNAP-tagged GHS-R1a expressed in HEK293T cells incubated at 4 degC for 3 hrs or at room temperature for 1 hr by Tag-lite assay
ChEMBL 661 17 6 8 4.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1 10.1016/j.bmcl.2016.04.003
56942099 125168 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645256 125168 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 599 13 3 7 5.0 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
66601728 81812 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 514 5 2 4 4.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
CHEMBL2164499 81812 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation countingDisplacement of [125I]-ghrelin from human GHSR1 expressed in CHO-CREluc cells after 1 hr by scintillation counting
ChEMBL 514 5 2 4 4.3 CCN1CCN(CC(=O)NC2(c3ccc(Cl)c(Cl)c3)C(=O)Nc3cc(Cl)cc(Cl)c32)CC1 10.1016/j.bmc.2012.07.018
162657465 181017 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 652 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc[nH]2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4759418 181017 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 652 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc[nH]2)cc1 10.1021/acs.jmedchem.9b02122
56926891 69032 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 520 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
CHEMBL1923635 69032 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 520 4 3 4 3.3 CC[C@H](C)[C@@H]1NCCCc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)N(C)C1=O 10.1021/jm2007062
44434015 88462 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 493 14 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCCc1ccccc1 10.1016/j.bmcl.2007.07.099
CHEMBL235011 88462 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 493 14 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCCc1ccccc1 10.1016/j.bmcl.2007.07.099
67407808 92254 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncc(C)cn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL2426687 92254 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIAInverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncc(C)cn5)ccc42)C3)nc1 10.1021/ml400473x
56926173 68983 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
CHEMBL1923501 68983 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O 10.1021/jm2007062
3153998 67491 3 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 480 13 2 3 5.5 CCCC(C(=O)NC1CCCCC1)N(CCCN(CC)CC)C(=O)c1ccc(-c2ccccc2)[nH]1 10.1021/jm040103i
CHEMBL189561 67491 3 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 480 13 2 3 5.5 CCCC(C(=O)NC1CCCCC1)N(CCCN(CC)CC)C(=O)c1ccc(-c2ccccc2)[nH]1 10.1021/jm040103i
56926893 69034 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 10.1021/jm2007062
CHEMBL1923637 69034 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assayDisplacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
ChEMBL 538 3 3 5 2.6 CC1COc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](C2CC2)N1 10.1021/jm2007062
66788278 125166 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3645254 125166 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 652 12 4 7 5.8 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1 10.1016/j.bmcl.2016.04.003
127045858 139837 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 618 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2=CCCCO2)cc1 10.1016/j.bmcl.2016.04.003
CHEMBL3799225 139837 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting methodDisplacement of [125I]-His9-ghrelin from human GHS-R1a transfected in pig LLC PK-1 cell membranes after 60 mins by gamma counting method
ChEMBL 618 12 3 7 5.3 COc1ccc(Cn2c([C@@H](Cc3ccccc3)NC(C)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2=CCCCO2)cc1 10.1016/j.bmcl.2016.04.003
162677268 183549 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 663 14 3 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4800459 183549 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 663 14 3 7 5.7 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccccc2)cc1 10.1021/acs.jmedchem.9b02122
58438487 92252 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 497 6 0 6 4.3 CCc1cnc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)Cc4ccc(OC)cn4)CC3)C2)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426685 92252 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 497 6 0 6 4.3 CCc1cnc(-c2ccc3c(c2)CC[C@H]3N2CC3(CCN(C(=O)Cc4ccc(OC)cn4)CC3)C2)nc1 10.1016/j.bmcl.2013.07.044
67407808 92254 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncc(C)cn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
CHEMBL2426687 92254 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation countingDisplacement of [125I]-ghrelin from human GHS-R1a expressed in tetracycline inducible HEK293 cells after 8 hrs by liquid scintillation counting
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncc(C)cn5)ccc42)C3)nc1 10.1016/j.bmcl.2013.07.044
67407808 92254 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncc(C)cn5)ccc42)C3)nc1 10.1021/ml400473x
CHEMBL2426687 92254 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assayDisplacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay
ChEMBL 483 5 0 6 4.0 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5ncc(C)cn5)ccc42)C3)nc1 10.1021/ml400473x
67406727 117166 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 525 6 1 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
CHEMBL3394201 117166 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA methodDisplacement of [125I]Ghrelin from human GHS-R1a expressed in HEK293 cells after 8 hrs by SPA method
ChEMBL 525 6 1 6 3.7 COc1ccc(CC(=O)N2CCC3(CC2)CN([C@@H]2CCc4cc(-c5cc(C)ncn5)ccc42)C3)c(C(N)=O)c1 10.1021/ml500414n
162656896 180836 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 669 14 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2cccs2)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4757313 180836 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 669 14 3 8 5.8 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2cccs2)cc1 10.1021/acs.jmedchem.9b02122
44579823 184057 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
CHEMBL482420 184057 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to GHSRBinding affinity to GHSR
ChEMBL 386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1cccc(Cl)c1 10.1016/j.bmcl.2008.07.120
44396320 66787 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 515 12 2 4 5.4 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccncc1 10.1021/jm040103i
CHEMBL186045 66787 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelinBinding affinity for human growth hormone secretagogue receptor was determined using [125I]ghrelin
ChEMBL 515 12 2 4 5.4 CCN(CC)CCCN(C(=O)c1ccc(-c2ccccc2)[nH]1)C(C(=O)NC1CCCCC1)c1ccncc1 10.1021/jm040103i
162674996 183365 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 522 12 3 6 4.2 CNCC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
CHEMBL4798018 183365 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assayDisplacement of red-ghrelin from SNAP-tagged human GHSR expressed in HEK293 cells incubated for 3 hrs at 4 degC or for 1 hr at room temperature by HTRF assay
ChEMBL 522 12 3 6 4.2 CNCC(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccc(OC)cc1 10.1021/acs.jmedchem.9b02122
44434111 146258 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1cc2ccccc2n1S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
CHEMBL392077 146258 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ghrelin from human GHSR1a after 1 hrDisplacement of [125I]ghrelin from human GHSR1a after 1 hr
ChEMBL 525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCc1cc2ccccc2n1S(C)(=O)=O 10.1016/j.bmcl.2007.07.099
9745 2437 20 None - 0 Human 8.1 pIC50 = 8.1 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Drug Central 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 None
9804938 2437 20 None - 0 Human 8.1 pIC50 = 8.1 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Drug Central 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 None
CHEMBL278623 2437 20 None - 0 Human 8.1 pIC50 = 8.1 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Drug Central 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 None
DB13074 2437 20 None - 0 Human 8.1 pIC50 = 8.1 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Drug Central 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 None
9745 2437 20 None - 0 Human 7.8 pIC50 = 7.8 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Guide to Pharmacology 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 12240910
9804938 2437 20 None - 0 Human 7.8 pIC50 = 7.8 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Guide to Pharmacology 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 12240910
CHEMBL278623 2437 20 None - 0 Human 7.8 pIC50 = 7.8 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Guide to Pharmacology 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 12240910
DB13074 2437 20 None - 0 Human 7.8 pIC50 = 7.8 Binding
In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.In a radioligand displacement assay using <sup>125</sup>I-labeled ghrelin as the probe, and human pituitary gland samples.
Guide to Pharmacology 474 10 6 4 1.8 O=CN[C@@H](Cc1c[nH]c2c1cccc2)NC(=O)[C@H](NC(=O)C(N)(C)C)Cc1c[nH]c2c1cccc2 12240910
1102 1309 0 None - 1 Human 7.4 pKd = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12907757
1093 1781 0 None -12 2 Human 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
1093 1781 0 None -12 2 Human 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
4345065 1781 0 None -12 2 Human 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
4345065 1781 0 None -12 2 Human 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
1100 1595 45 None - 1 Human 7.9 pKd = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11061542
6918297 1595 45 None - 1 Human 7.9 pKd = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11061542
CHEMBL108335 1595 45 None - 1 Human 7.9 pKd = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11061542
1099 1773 0 None - 1 Human 9.0 pKd = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12907757
1099 1773 0 None - 1 Human 9.0 pKd = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15905359
1092 3136 0 None - 1 Rat 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
134715446 3136 0 None - 1 Rat 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
2232 3136 0 None - 1 Rat 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
6918245 3136 0 None - 1 Rat 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
CHEMBL106593 3136 0 None - 1 Rat 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
58438464 3043 35 None -2 3 Mouse 8.1 pKi = 8.1 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
9060 3043 35 None -2 3 Mouse 8.1 pKi = 8.1 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
CHEMBL3287218 3043 35 None -2 3 Mouse 8.1 pKi = 8.1 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
DB14870 3043 35 None -2 3 Mouse 8.1 pKi = 8.1 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
58438464 3043 35 None -1 3 Rat 8.5 pKi = 8.5 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
9060 3043 35 None -1 3 Rat 8.5 pKi = 8.5 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
CHEMBL3287218 3043 35 None -1 3 Rat 8.5 pKi = 8.5 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
DB14870 3043 35 None -1 3 Rat 8.5 pKi = 8.5 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cellsMeasured <i>in vitro</i> in recombinant receptor over-expressing cells
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
58438464 3043 35 None 1 3 Human 8.9 pKi = 8.9 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cells.Measured <i>in vitro</i> in recombinant receptor over-expressing cells.
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
9060 3043 35 None 1 3 Human 8.9 pKi = 8.9 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cells.Measured <i>in vitro</i> in recombinant receptor over-expressing cells.
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
CHEMBL3287218 3043 35 None 1 3 Human 8.9 pKi = 8.9 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cells.Measured <i>in vitro</i> in recombinant receptor over-expressing cells.
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
DB14870 3043 35 None 1 3 Human 8.9 pKi = 8.9 Binding
Measured <i>in vitro</i> in recombinant receptor over-expressing cells.Measured <i>in vitro</i> in recombinant receptor over-expressing cells.
Guide to Pharmacology 512 4 0 7 4.6 Cc1ncnc(c1)c1ccc2c(c1)CC[C@H]2N1CC2(C1)CCN(CC2)C(=O)Cc1nc2n(c1)cc(s2)C 26784385
12413 3048 0 None -3 2 Rat 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 4 1 8 4.3 CC1=CN2C=C(CC(=O)N3CCC4(CN(C4)[C@@H]5CCC6=CC(=CC=C56)C7=CC(C)=NC(O)=N7)CC3)N=C2S1 36631279
164946906 3048 0 None -3 2 Rat 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 4 1 8 4.3 CC1=CN2C=C(CC(=O)N3CCC4(CN(C4)[C@@H]5CCC6=CC(=CC=C56)C7=CC(C)=NC(O)=N7)CC3)N=C2S1 36631279
12413 3048 0 None 3 2 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 4 1 8 4.3 CC1=CN2C=C(CC(=O)N3CCC4(CN(C4)[C@@H]5CCC6=CC(=CC=C56)C7=CC(C)=NC(O)=N7)CC3)N=C2S1 36631279
164946906 3048 0 None 3 2 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 4 1 8 4.3 CC1=CN2C=C(CC(=O)N3CCC4(CN(C4)[C@@H]5CCC6=CC(=CC=C56)C7=CC(C)=NC(O)=N7)CC3)N=C2S1 36631279
23631116 4081 23 None - 1 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 5 0 5 4.8 Fc1ccc(cc1)Oc1ccc2c(c1)c(=O)n(c(n2)C)C[C@H]1CCCN(C1)C(C)C 17656463
3538 4081 23 None - 1 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 5 0 5 4.8 Fc1ccc(cc1)Oc1ccc2c(c1)c(=O)n(c(n2)C)C[C@H]1CCCN(C1)C(C)C 17656463
CHEMBL243001 4081 23 None - 1 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 5 0 5 4.8 Fc1ccc(cc1)Oc1ccc2c(c1)c(=O)n(c(n2)C)C[C@H]1CCCN(C1)C(C)C 17656463
1098 1379 0 None - 1 Rat 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11314756
1098 1379 0 None - 1 Rat 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14763915
1101 654 0 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15339248
10740 1925 0 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 4 1 3 4.4 COc1ccc(c(c1Cl)Cl)[C@@H](NC(=O)N([C@@H]1CCN(CC1(C)C)C)C)C 25327342
146170991 1925 0 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 4 1 3 4.4 COc1ccc(c(c1Cl)Cl)[C@@H](NC(=O)N([C@@H]1CCN(CC1(C)C)C)C)C 25327342
1092 3136 0 None - 1 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
134715446 3136 0 None - 1 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
2232 3136 0 None - 1 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
6918245 3136 0 None - 1 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
CHEMBL106593 3136 0 None - 1 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
178024 1958 33 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10427162
5867 1958 33 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10427162
CHEMBL13817 1958 33 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C 10427162
1099 1773 0 None - 1 Human 8.0 pKi None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11314756
1093 1781 0 None 12 2 Rat 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793
4345065 1781 0 None 12 2 Rat 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9092793