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Ligand source activities (1 row/activity)

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Ligand Receptor Assay information Chemical information
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44570962 182980 0 GHSR ghrelin receptor 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 182980 0 GHSR ghrelin receptor 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 162002 0 GHSR ghrelin receptor 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 162002 0 GHSR ghrelin receptor 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
CHEMBL4641513 176806 0 GHSR ghrelin receptor 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 93823 0 GHSR ghrelin receptor 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 93823 0 GHSR ghrelin receptor 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
CHEMBL4635542 176372 0 GHSR ghrelin receptor 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
CHEMBL4641513 176806 0 GHSR ghrelin receptor 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 93823 0 GHSR ghrelin receptor 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 93823 0 GHSR ghrelin receptor 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 183003 0 GHSR ghrelin receptor 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 183003 0 GHSR ghrelin receptor 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
CHEMBL4635542 176372 0 GHSR ghrelin receptor 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
178024 1843 22 GHSR ghrelin receptor 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 1843 22 GHSR ghrelin receptor 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 1843 22 GHSR ghrelin receptor 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
44444563 154148 0 GHSR ghrelin receptor 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 154148 0 GHSR ghrelin receptor 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
CHEMBL4638297 176549 0 GHSR ghrelin receptor 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 187229 0 GHSR ghrelin receptor 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 187229 0 GHSR ghrelin receptor 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 95209 0 GHSR ghrelin receptor 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 95209 0 GHSR ghrelin receptor 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 158573 0 GHSR ghrelin receptor 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 158573 0 GHSR ghrelin receptor 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 158587 0 GHSR ghrelin receptor 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 158587 0 GHSR ghrelin receptor 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
CHEMBL4638297 176549 0 GHSR ghrelin receptor 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
CHEMBL4643530 176955 0 GHSR ghrelin receptor 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
CHEMBL4640507 176721 0 GHSR ghrelin receptor 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
CHEMBL4643530 176955 0 GHSR ghrelin receptor 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 183112 0 GHSR ghrelin receptor 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 183112 0 GHSR ghrelin receptor 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 175946 0 GHSR ghrelin receptor 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 175946 0 GHSR ghrelin receptor 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
CHEMBL4640507 176721 0 GHSR ghrelin receptor 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 10049 0 GHSR ghrelin receptor 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 10049 0 GHSR ghrelin receptor 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 10049 0 GHSR ghrelin receptor 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 10049 0 GHSR ghrelin receptor 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 96880 0 GHSR ghrelin receptor 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 96880 0 GHSR ghrelin receptor 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
CHEMBL4647963 177254 0 GHSR ghrelin receptor 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 183173 0 GHSR ghrelin receptor 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 183173 0 GHSR ghrelin receptor 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 88339 0 GHSR ghrelin receptor 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 88339 0 GHSR ghrelin receptor 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
CHEMBL4647963 177254 0 GHSR ghrelin receptor 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 108991 0 GHSR ghrelin receptor 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 108991 0 GHSR ghrelin receptor 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 188455 0 GHSR ghrelin receptor 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 188455 0 GHSR ghrelin receptor 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 1843 22 GHSR ghrelin receptor 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 1843 22 GHSR ghrelin receptor 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 1843 22 GHSR ghrelin receptor 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
CHEMBL4639111 176621 0 GHSR ghrelin receptor 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
CHEMBL4639229 176633 0 GHSR ghrelin receptor 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 95528 0 GHSR ghrelin receptor 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 95528 0 GHSR ghrelin receptor 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 187293 0 GHSR ghrelin receptor 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 187293 0 GHSR ghrelin receptor 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 88297 0 GHSR ghrelin receptor 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 88297 0 GHSR ghrelin receptor 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 1843 22 GHSR ghrelin receptor 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 1843 22 GHSR ghrelin receptor 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 1843 22 GHSR ghrelin receptor 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 97112 0 GHSR ghrelin receptor 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 97112 0 GHSR ghrelin receptor 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 154795 0 GHSR ghrelin receptor 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 154795 0 GHSR ghrelin receptor 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 94309 0 GHSR ghrelin receptor 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 94309 0 GHSR ghrelin receptor 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
CHEMBL4639111 176621 0 GHSR ghrelin receptor 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
CHEMBL4639229 176633 0 GHSR ghrelin receptor 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 166050 0 GHSR ghrelin receptor 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 166050 0 GHSR ghrelin receptor 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
CHEMBL4646219 177140 0 GHSR ghrelin receptor 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 62910 0 GHSR ghrelin receptor 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 62910 0 GHSR ghrelin receptor 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 63087 0 GHSR ghrelin receptor 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 63087 0 GHSR ghrelin receptor 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 63087 0 GHSR ghrelin receptor 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 63087 0 GHSR ghrelin receptor 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 63087 0 GHSR ghrelin receptor 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 63087 0 GHSR ghrelin receptor 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 122043 0 GHSR ghrelin receptor 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 122043 0 GHSR ghrelin receptor 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 122043 0 GHSR ghrelin receptor 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 122043 0 GHSR ghrelin receptor 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 154748 0 GHSR ghrelin receptor 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 154748 0 GHSR ghrelin receptor 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 93760 0 GHSR ghrelin receptor 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 93760 0 GHSR ghrelin receptor 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
CHEMBL4636502 176439 0 GHSR ghrelin receptor 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
CHEMBL4646219 177140 0 GHSR ghrelin receptor 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 97297 0 GHSR ghrelin receptor 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 97297 0 GHSR ghrelin receptor 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 182692 0 GHSR ghrelin receptor 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 182692 0 GHSR ghrelin receptor 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 88299 0 GHSR ghrelin receptor 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 88299 0 GHSR ghrelin receptor 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 88344 0 GHSR ghrelin receptor 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 88344 0 GHSR ghrelin receptor 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 154754 0 GHSR ghrelin receptor 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 154754 0 GHSR ghrelin receptor 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
CHEMBL4636502 176439 0 GHSR ghrelin receptor 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
22867441 10038 0 GHSR ghrelin receptor 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 10038 0 GHSR ghrelin receptor 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 91160 0 GHSR ghrelin receptor 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 91160 0 GHSR ghrelin receptor 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
44450016 159735 0 GHSR ghrelin receptor 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 159735 0 GHSR ghrelin receptor 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 94576 0 GHSR ghrelin receptor 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 94576 0 GHSR ghrelin receptor 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 10038 0 GHSR ghrelin receptor 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 10038 0 GHSR ghrelin receptor 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 78513 0 GHSR ghrelin receptor 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 78513 0 GHSR ghrelin receptor 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 10038 0 GHSR ghrelin receptor 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 10038 0 GHSR ghrelin receptor 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
22867441 10038 0 GHSR ghrelin receptor 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 10038 0 GHSR ghrelin receptor 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 154271 0 GHSR ghrelin receptor 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 154271 0 GHSR ghrelin receptor 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 88223 0 GHSR ghrelin receptor 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 88223 0 GHSR ghrelin receptor 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 158635 0 GHSR ghrelin receptor 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 158635 0 GHSR ghrelin receptor 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 131003 0 GHSR ghrelin receptor 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 131003 0 GHSR ghrelin receptor 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 160276 0 GHSR ghrelin receptor 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 160276 0 GHSR ghrelin receptor 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 94337 0 GHSR ghrelin receptor 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 94337 0 GHSR ghrelin receptor 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 62539 0 GHSR ghrelin receptor 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 62539 0 GHSR ghrelin receptor 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
CHEMBL4647797 177238 0 GHSR ghrelin receptor 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
71716660 85335 0 GHSR ghrelin receptor 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 85335 0 GHSR ghrelin receptor 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 138480 0 GHSR ghrelin receptor 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 138480 0 GHSR ghrelin receptor 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
44444571 93306 0 GHSR ghrelin receptor 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 93306 0 GHSR ghrelin receptor 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 103843 0 GHSR ghrelin receptor 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 103843 0 GHSR ghrelin receptor 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 138480 0 GHSR ghrelin receptor 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 138480 0 GHSR ghrelin receptor 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
CHEMBL4637980 176530 0 GHSR ghrelin receptor 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
CHEMBL4647797 177238 0 GHSR ghrelin receptor 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 97339 0 GHSR ghrelin receptor 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 97339 0 GHSR ghrelin receptor 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 156484 0 GHSR ghrelin receptor 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 156484 0 GHSR ghrelin receptor 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 156484 0 GHSR ghrelin receptor 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 156484 0 GHSR ghrelin receptor 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 88277 0 GHSR ghrelin receptor 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 88277 0 GHSR ghrelin receptor 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
71716660 85335 0 GHSR ghrelin receptor 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 85335 0 GHSR ghrelin receptor 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 138480 0 GHSR ghrelin receptor 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 138480 0 GHSR ghrelin receptor 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
44454060 154525 0 GHSR ghrelin receptor 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 154525 0 GHSR ghrelin receptor 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 103843 0 GHSR ghrelin receptor 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 103843 0 GHSR ghrelin receptor 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 138480 0 GHSR ghrelin receptor 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 138480 0 GHSR ghrelin receptor 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 138973 0 GHSR ghrelin receptor 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 138973 0 GHSR ghrelin receptor 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
CHEMBL4649634 177355 0 GHSR ghrelin receptor 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
CHEMBL4637980 176530 0 GHSR ghrelin receptor 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 62902 0 GHSR ghrelin receptor 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 62902 0 GHSR ghrelin receptor 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 178237 0 GHSR ghrelin receptor 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 178237 0 GHSR ghrelin receptor 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 9455 21 GHSR ghrelin receptor 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 9455 21 GHSR ghrelin receptor 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 95787 0 GHSR ghrelin receptor 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 95787 0 GHSR ghrelin receptor 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 9455 21 GHSR ghrelin receptor 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 9455 21 GHSR ghrelin receptor 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
CHEMBL4647258 177204 0 GHSR ghrelin receptor 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
9807597 182141 2 GHSR ghrelin receptor 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 182141 2 GHSR ghrelin receptor 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
44437955 10047 0 GHSR ghrelin receptor 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 10047 0 GHSR ghrelin receptor 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 182141 2 GHSR ghrelin receptor 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 182141 2 GHSR ghrelin receptor 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
CHEMBL4645148 177062 0 GHSR ghrelin receptor 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
CHEMBL4647258 177204 0 GHSR ghrelin receptor 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
CHEMBL4649603 177352 0 GHSR ghrelin receptor 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
CHEMBL4649634 177355 0 GHSR ghrelin receptor 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 68440 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 68440 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 68446 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 68446 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 68464 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 68464 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 68465 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 68465 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 68472 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 68472 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 68481 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 68481 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 68492 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 68492 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 68496 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 68496 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 71025 9 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 71025 9 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 71025 9 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 141573 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 141573 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 142024 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 142024 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 142335 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 142335 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 142651 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 142651 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 142703 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 142703 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 142892 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 142892 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 143336 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 143336 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 143566 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 143566 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 143763 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 143763 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144060 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144060 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144129 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144129 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144484 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144484 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144523 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144523 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144583 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144583 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144771 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144771 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144958 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 144958 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145135 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145135 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145390 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145390 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145572 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145572 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145646 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145646 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145753 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 145753 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 146317 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 146317 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 146949 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 146949 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 146952 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 146952 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 147213 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 147213 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 147553 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 147553 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 147673 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 147673 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 147985 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 147985 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 148289 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 148289 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 148688 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 148688 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 150212 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 150212 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 150290 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 150290 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 151601 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 151601 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 151919 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 151919 0 GHSR ghrelin receptor Human 9.0 pEC50 = 9 Functional
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release 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 187094 0 GHSR ghrelin receptor 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 187094 0 GHSR ghrelin receptor 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 89070 0 GHSR ghrelin receptor 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 89070 0 GHSR ghrelin receptor 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 88207 0 GHSR ghrelin receptor 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 88207 0 GHSR ghrelin receptor 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 88222 0 GHSR ghrelin receptor 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 88222 0 GHSR ghrelin receptor 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 88251 0 GHSR ghrelin receptor 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 88251 0 GHSR ghrelin receptor 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 88272 0 GHSR ghrelin receptor 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 88272 0 GHSR ghrelin receptor 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 160988 0 GHSR ghrelin receptor 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 160988 0 GHSR ghrelin receptor 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
CHEMBL4645148 177062 0 GHSR ghrelin receptor 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
CHEMBL4649603 177352 0 GHSR ghrelin receptor 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 10032 0 GHSR ghrelin receptor 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 10032 0 GHSR ghrelin receptor 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 10032 0 GHSR ghrelin receptor 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 10032 0 GHSR ghrelin receptor 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 10032 0 GHSR ghrelin receptor 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 10032 0 GHSR ghrelin receptor 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 10032 0 GHSR ghrelin receptor 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 10032 0 GHSR ghrelin receptor 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 94282 0 GHSR ghrelin receptor 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 94282 0 GHSR ghrelin receptor 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 154755 0 GHSR ghrelin receptor 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 154755 0 GHSR ghrelin receptor 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 26935 0 GHSR ghrelin receptor 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 26935 0 GHSR ghrelin receptor 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 97648 0 GHSR ghrelin receptor 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 97648 0 GHSR ghrelin receptor 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 161868 0 GHSR ghrelin receptor 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 161868 0 GHSR ghrelin receptor 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 186988 0 GHSR ghrelin receptor 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 186988 0 GHSR ghrelin receptor 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 88294 0 GHSR ghrelin receptor 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 88294 0 GHSR ghrelin receptor 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 88303 0 GHSR ghrelin receptor 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 88303 0 GHSR ghrelin receptor 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 94253 0 GHSR ghrelin receptor 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 94253 0 GHSR ghrelin receptor 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
44411920 77287 0 GHSR ghrelin receptor 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 77287 0 GHSR ghrelin receptor 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
CHEMBL4765101 180648 0 GHSR ghrelin receptor 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 108573 0 GHSR ghrelin receptor 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 108573 0 GHSR ghrelin receptor 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
44450015 95631 0 GHSR ghrelin receptor 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 95631 0 GHSR ghrelin receptor 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 1843 22 GHSR ghrelin receptor 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 1843 22 GHSR ghrelin receptor 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 1843 22 GHSR ghrelin receptor 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 1843 22 GHSR ghrelin receptor 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 1843 22 GHSR ghrelin receptor 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 1843 22 GHSR ghrelin receptor 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
44411920 77287 0 GHSR ghrelin receptor 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 77287 0 GHSR ghrelin receptor 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
178024 1843 22 GHSR ghrelin receptor 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 1843 22 GHSR ghrelin receptor 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 1843 22 GHSR ghrelin receptor 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 161868 0 GHSR ghrelin receptor 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 161868 0 GHSR ghrelin receptor 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 95117 0 GHSR ghrelin receptor 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 95117 0 GHSR ghrelin receptor 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 207539 0 GHSR ghrelin receptor 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 207539 0 GHSR ghrelin receptor 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 63269 0 GHSR ghrelin receptor 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 63269 0 GHSR ghrelin receptor 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 207539 0 GHSR ghrelin receptor 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
CHEMBL4753794 179676 0 GHSR ghrelin receptor 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 207539 0 GHSR ghrelin receptor 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 207539 0 GHSR ghrelin receptor 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 1843 22 GHSR ghrelin receptor 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 1843 22 GHSR ghrelin receptor 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 1843 22 GHSR ghrelin receptor 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
CHEMBL4636571 176447 0 GHSR ghrelin receptor 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 63748 0 GHSR ghrelin receptor 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 63748 0 GHSR ghrelin receptor 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 64060 0 GHSR ghrelin receptor 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 64060 0 GHSR ghrelin receptor 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 64060 0 GHSR ghrelin receptor 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 64060 0 GHSR ghrelin receptor 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 16014 0 GHSR ghrelin receptor 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 16014 0 GHSR ghrelin receptor 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 206843 15 GHSR ghrelin receptor 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 206843 15 GHSR ghrelin receptor 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
10625750 167320 0 GHSR ghrelin receptor 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 167320 0 GHSR ghrelin receptor 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
145957574 161476 0 GHSR ghrelin receptor 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 161476 0 GHSR ghrelin receptor 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 198860 0 GHSR ghrelin receptor 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 198860 0 GHSR ghrelin receptor 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
CHEMBL4636571 176447 0 GHSR ghrelin receptor 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
CHEMBL4639379 176638 0 GHSR ghrelin receptor 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 88250 0 GHSR ghrelin receptor 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 88250 0 GHSR ghrelin receptor 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 88253 0 GHSR ghrelin receptor 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 88253 0 GHSR ghrelin receptor 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 88296 0 GHSR ghrelin receptor 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 88296 0 GHSR ghrelin receptor 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 88301 0 GHSR ghrelin receptor 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 88301 0 GHSR ghrelin receptor 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 88347 0 GHSR ghrelin receptor 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 88347 0 GHSR ghrelin receptor 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
10625750 167320 0 GHSR ghrelin receptor 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 167320 0 GHSR ghrelin receptor 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
16114292 96246 0 GHSR ghrelin receptor 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 96246 0 GHSR ghrelin receptor 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 198860 0 GHSR ghrelin receptor 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 198860 0 GHSR ghrelin receptor 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 90877 0 GHSR ghrelin receptor 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 90877 0 GHSR ghrelin receptor 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 94310 0 GHSR ghrelin receptor 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 94310 0 GHSR ghrelin receptor 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 94283 0 GHSR ghrelin receptor 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 94283 0 GHSR ghrelin receptor 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 201995 32 GHSR ghrelin receptor 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 94195 0 GHSR ghrelin receptor 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 94195 0 GHSR ghrelin receptor 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 95659 0 GHSR ghrelin receptor 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 95659 0 GHSR ghrelin receptor 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 23700 0 GHSR ghrelin receptor 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 23700 0 GHSR ghrelin receptor 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 27090 0 GHSR ghrelin receptor 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 27090 0 GHSR ghrelin receptor 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 112248 0 GHSR ghrelin receptor 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 112248 0 GHSR ghrelin receptor 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 23700 0 GHSR ghrelin receptor 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 23700 0 GHSR ghrelin receptor 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
CHEMBL4632657 176203 0 GHSR ghrelin receptor 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 153165 4 GHSR ghrelin receptor 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 153165 4 GHSR ghrelin receptor 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 153165 4 GHSR ghrelin receptor 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 153165 4 GHSR ghrelin receptor 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 153165 4 GHSR ghrelin receptor 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 153165 4 GHSR ghrelin receptor 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 153165 4 GHSR ghrelin receptor 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 153165 4 GHSR ghrelin receptor 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
10626337 100515 0 GHSR ghrelin receptor 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 100515 0 GHSR ghrelin receptor 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
44437955 10047 0 GHSR ghrelin receptor 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 10047 0 GHSR ghrelin receptor 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 100515 0 GHSR ghrelin receptor 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 100515 0 GHSR ghrelin receptor 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
CHEMBL4632657 176203 0 GHSR ghrelin receptor 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
CHEMBL4637284 176484 0 GHSR ghrelin receptor 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
CHEMBL4640615 176730 0 GHSR ghrelin receptor 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 95570 0 GHSR ghrelin receptor 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 95570 0 GHSR ghrelin receptor 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 96898 0 GHSR ghrelin receptor 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 96898 0 GHSR ghrelin receptor 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 183083 0 GHSR ghrelin receptor 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 183083 0 GHSR ghrelin receptor 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 88268 0 GHSR ghrelin receptor 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 88268 0 GHSR ghrelin receptor 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 88276 0 GHSR ghrelin receptor 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 88276 0 GHSR ghrelin receptor 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 88312 0 GHSR ghrelin receptor 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 88312 0 GHSR ghrelin receptor 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 88352 0 GHSR ghrelin receptor 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 88352 0 GHSR ghrelin receptor 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
44411718 10029 0 GHSR ghrelin receptor 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 10029 0 GHSR ghrelin receptor 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 100379 0 GHSR ghrelin receptor 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 100379 0 GHSR ghrelin receptor 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 100379 0 GHSR ghrelin receptor 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
44579802 184091 0 GHSR ghrelin receptor 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 184091 0 GHSR ghrelin receptor 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 93346 0 GHSR ghrelin receptor 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 93346 0 GHSR ghrelin receptor 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 161250 0 GHSR ghrelin receptor 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 161250 0 GHSR ghrelin receptor 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 161951 0 GHSR ghrelin receptor 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 161951 0 GHSR ghrelin receptor 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 89237 0 GHSR ghrelin receptor 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 89237 0 GHSR ghrelin receptor 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 5084 0 GHSR ghrelin receptor 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 5084 0 GHSR ghrelin receptor 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 10029 0 GHSR ghrelin receptor 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 10029 0 GHSR ghrelin receptor 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 10046 0 GHSR ghrelin receptor 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 10046 0 GHSR ghrelin receptor 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 100379 0 GHSR ghrelin receptor 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 100379 0 GHSR ghrelin receptor 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 100379 0 GHSR ghrelin receptor 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 138986 0 GHSR ghrelin receptor 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 138986 0 GHSR ghrelin receptor 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
CHEMBL4637255 176483 0 GHSR ghrelin receptor 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
CHEMBL4641201 176779 0 GHSR ghrelin receptor 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 94696 0 GHSR ghrelin receptor 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 94696 0 GHSR ghrelin receptor 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 183170 0 GHSR ghrelin receptor 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 183170 0 GHSR ghrelin receptor 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 201995 32 GHSR ghrelin receptor 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 88212 0 GHSR ghrelin receptor 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 88212 0 GHSR ghrelin receptor 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 88227 0 GHSR ghrelin receptor 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 88227 0 GHSR ghrelin receptor 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 88228 0 GHSR ghrelin receptor 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 88228 0 GHSR ghrelin receptor 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 88246 0 GHSR ghrelin receptor 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 88246 0 GHSR ghrelin receptor 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 88259 0 GHSR ghrelin receptor 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 88259 0 GHSR ghrelin receptor 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 88302 0 GHSR ghrelin receptor 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 88302 0 GHSR ghrelin receptor 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 88315 0 GHSR ghrelin receptor 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 88315 0 GHSR ghrelin receptor 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 88349 0 GHSR ghrelin receptor 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 88349 0 GHSR ghrelin receptor 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 88351 0 GHSR ghrelin receptor 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 88351 0 GHSR ghrelin receptor 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 147318 0 GHSR ghrelin receptor 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 147318 0 GHSR ghrelin receptor 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
CHEMBL4641201 176779 0 GHSR ghrelin receptor 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 166492 0 GHSR ghrelin receptor 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 166492 0 GHSR ghrelin receptor 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
CHEMBL4637255 176483 0 GHSR ghrelin receptor 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
16040587 178519 0 GHSR ghrelin receptor 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 178519 0 GHSR ghrelin receptor 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
145950201 162117 0 GHSR ghrelin receptor 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 162117 0 GHSR ghrelin receptor 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 168543 0 GHSR ghrelin receptor 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 168543 0 GHSR ghrelin receptor 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 95995 0 GHSR ghrelin receptor 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 95995 0 GHSR ghrelin receptor 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 97125 0 GHSR ghrelin receptor 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 97125 0 GHSR ghrelin receptor 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 158510 0 GHSR ghrelin receptor 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 158510 0 GHSR ghrelin receptor 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 68483 0 GHSR ghrelin receptor 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 68483 0 GHSR ghrelin receptor 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 68485 0 GHSR ghrelin receptor 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 68485 0 GHSR ghrelin receptor 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 68488 0 GHSR ghrelin receptor 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 68488 0 GHSR ghrelin receptor 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 68490 0 GHSR ghrelin receptor 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 68490 0 GHSR ghrelin receptor 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 68491 0 GHSR ghrelin receptor 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 68491 0 GHSR ghrelin receptor 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 141667 0 GHSR ghrelin receptor 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 141667 0 GHSR ghrelin receptor 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 142434 0 GHSR ghrelin receptor 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 142434 0 GHSR ghrelin receptor 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 143589 0 GHSR ghrelin receptor 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 143589 0 GHSR ghrelin receptor 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 143858 0 GHSR ghrelin receptor 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 143858 0 GHSR ghrelin receptor 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 144168 0 GHSR ghrelin receptor 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 144168 0 GHSR ghrelin receptor 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 144657 0 GHSR ghrelin receptor 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 144657 0 GHSR ghrelin receptor 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 145928 0 GHSR ghrelin receptor 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 145928 0 GHSR ghrelin receptor 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 147652 0 GHSR ghrelin receptor 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 147652 0 GHSR ghrelin receptor 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 147979 0 GHSR ghrelin receptor 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 147979 0 GHSR ghrelin receptor 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 148233 0 GHSR ghrelin receptor 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 148233 0 GHSR ghrelin receptor 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 150210 0 GHSR ghrelin receptor 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 150210 0 GHSR ghrelin receptor 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 150540 0 GHSR ghrelin receptor 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 150540 0 GHSR ghrelin receptor 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 150746 0 GHSR ghrelin receptor 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 150746 0 GHSR ghrelin receptor 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 151277 0 GHSR ghrelin receptor 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 151277 0 GHSR ghrelin receptor 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 151313 0 GHSR ghrelin receptor 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 151313 0 GHSR ghrelin receptor 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 151568 0 GHSR ghrelin receptor 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 151568 0 GHSR ghrelin receptor 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 152024 0 GHSR ghrelin receptor 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 152024 0 GHSR ghrelin receptor 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 152517 0 GHSR ghrelin receptor 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 152517 0 GHSR ghrelin receptor 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 152849 0 GHSR ghrelin receptor 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 152849 0 GHSR ghrelin receptor 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 178519 0 GHSR ghrelin receptor 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 178519 0 GHSR ghrelin receptor 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
16040587 178519 0 GHSR ghrelin receptor 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 178519 0 GHSR ghrelin receptor 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
44576247 207641 0 GHSR ghrelin receptor 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 207641 0 GHSR ghrelin receptor 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 205280 0 GHSR ghrelin receptor 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 205283 0 GHSR ghrelin receptor 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 88233 0 GHSR ghrelin receptor 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 88233 0 GHSR ghrelin receptor 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 88235 0 GHSR ghrelin receptor 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 88235 0 GHSR ghrelin receptor 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 88244 0 GHSR ghrelin receptor 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 88244 0 GHSR ghrelin receptor 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 88245 0 GHSR ghrelin receptor 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 88245 0 GHSR ghrelin receptor 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 88266 0 GHSR ghrelin receptor 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 88266 0 GHSR ghrelin receptor 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 88283 0 GHSR ghrelin receptor 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 88283 0 GHSR ghrelin receptor 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 88287 0 GHSR ghrelin receptor 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 88287 0 GHSR ghrelin receptor 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 88305 0 GHSR ghrelin receptor 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 88305 0 GHSR ghrelin receptor 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 88334 0 GHSR ghrelin receptor 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 88334 0 GHSR ghrelin receptor 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 187271 0 GHSR ghrelin receptor 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 187271 0 GHSR ghrelin receptor 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
CHEMBL4647751 177237 0 GHSR ghrelin receptor 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 145234 0 GHSR ghrelin receptor 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 145234 0 GHSR ghrelin receptor 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 95651 0 GHSR ghrelin receptor 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 95651 0 GHSR ghrelin receptor 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
CHEMBL4647751 177237 0 GHSR ghrelin receptor 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 87844 0 GHSR ghrelin receptor 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 87844 0 GHSR ghrelin receptor 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 205283 0 GHSR ghrelin receptor 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 95087 0 GHSR ghrelin receptor 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 95087 0 GHSR ghrelin receptor 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 136420 0 GHSR ghrelin receptor 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 136420 0 GHSR ghrelin receptor 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 68481 0 GHSR ghrelin receptor 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 68481 0 GHSR ghrelin receptor 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 202891 9 GHSR ghrelin receptor 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 202891 9 GHSR ghrelin receptor 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 63758 0 GHSR ghrelin receptor 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 63758 0 GHSR ghrelin receptor 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 88745 0 GHSR ghrelin receptor 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 88745 0 GHSR ghrelin receptor 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 146058 0 GHSR ghrelin receptor 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 146058 0 GHSR ghrelin receptor 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 166435 0 GHSR ghrelin receptor 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 166435 0 GHSR ghrelin receptor 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 202886 0 GHSR ghrelin receptor 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 89360 0 GHSR ghrelin receptor 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 89360 0 GHSR ghrelin receptor 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 90880 0 GHSR ghrelin receptor 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 90880 0 GHSR ghrelin receptor 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 140810 0 GHSR ghrelin receptor 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 140810 0 GHSR ghrelin receptor 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 93999 0 GHSR ghrelin receptor 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 93999 0 GHSR ghrelin receptor 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 63762 0 GHSR ghrelin receptor 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 63762 0 GHSR ghrelin receptor 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 202891 9 GHSR ghrelin receptor 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 202891 9 GHSR ghrelin receptor 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
CHEMBL4643595 176958 0 GHSR ghrelin receptor 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 162109 0 GHSR ghrelin receptor 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 162109 0 GHSR ghrelin receptor 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
CHEMBL4635743 176389 0 GHSR ghrelin receptor 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
CHEMBL4643595 176958 0 GHSR ghrelin receptor 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 88205 0 GHSR ghrelin receptor 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 88205 0 GHSR ghrelin receptor 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 88256 0 GHSR ghrelin receptor 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 88256 0 GHSR ghrelin receptor 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 88288 0 GHSR ghrelin receptor 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 88288 0 GHSR ghrelin receptor 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 88304 0 GHSR ghrelin receptor 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 88304 0 GHSR ghrelin receptor 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 88322 0 GHSR ghrelin receptor 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 88322 0 GHSR ghrelin receptor 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 88329 0 GHSR ghrelin receptor 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 88329 0 GHSR ghrelin receptor 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 88355 0 GHSR ghrelin receptor 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 88355 0 GHSR ghrelin receptor 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 88358 0 GHSR ghrelin receptor 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 88358 0 GHSR ghrelin receptor 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 202889 0 GHSR ghrelin receptor 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 183234 0 GHSR ghrelin receptor 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 183234 0 GHSR ghrelin receptor 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 184160 0 GHSR ghrelin receptor 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 184160 0 GHSR ghrelin receptor 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 188186 0 GHSR ghrelin receptor 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 188186 0 GHSR ghrelin receptor 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 187612 0 GHSR ghrelin receptor 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 187612 0 GHSR ghrelin receptor 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 165924 0 GHSR ghrelin receptor 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 165924 0 GHSR ghrelin receptor 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
CHEMBL4642860 176915 0 GHSR ghrelin receptor 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 202887 0 GHSR ghrelin receptor 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 185689 0 GHSR ghrelin receptor 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 185689 0 GHSR ghrelin receptor 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
16752689 185689 0 GHSR ghrelin receptor 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 185689 0 GHSR ghrelin receptor 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
44444557 153880 0 GHSR ghrelin receptor 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 153880 0 GHSR ghrelin receptor 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