Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Unit Assay Type Assay Description Mol
weight
Rot
Bonds
H don H acc LogP Smiles
CHEMBL480821 ghsr_human Human No 10.3 EC50 = 0.1 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
435 4 1 5 2.5 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1
CHEMBL4172656 ghsr_human Human No 10.0 EC50 = 0.1 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
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
CHEMBL4641513 ghsr_human Human No 9.8 EC50 = 0.1 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL251572 ghsr_human Human No 9.8 EC50 = 0.2 nM Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
484 5 1 7 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2
CHEMBL4635542 ghsr_human Human No 9.8 EC50 = 0.2 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4641513 ghsr_human Human No 9.8 EC50 = 0.2 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL251572 ghsr_human Human No 9.8 EC50 = 0.2 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
484 5 1 7 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2
CHEMBL481013 ghsr_human Human No 9.8 EC50 = 0.2 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
435 4 1 5 2.5 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@H](N)C3)cc2F)o1
CHEMBL4635542 ghsr_human Human No 9.8 EC50 = 0.2 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL13817 ghsr_human Human Yes 9.7 EC50 = 0.2 nM Bind
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C
CHEMBL401134 ghsr_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
478 5 1 6 3.7 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)cc1)CC2
CHEMBL4638297 ghsr_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL518774 ghsr_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
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
CHEMBL259166 ghsr_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
493 16 4 10 0.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCSCCO
CHEMBL410074 ghsr_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
525 16 4 11 -0.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCS(=O)(=O)CCO
CHEMBL410085 ghsr_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
509 14 4 9 1.6 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1cccc(O)c1
CHEMBL4638297 ghsr_human Human No 9.7 EC50 = 0.2 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4643530 ghsr_human Human No 9.6 EC50 = 0.2 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4640507 ghsr_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4643530 ghsr_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL481796 ghsr_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
417 4 1 5 2.4 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2)o1
CHEMBL460680 ghsr_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at GHS receptorAgonist activity at GHS receptor
497 14 4 9 1.6 CC(C)(N)C(=O)N[C@H](CCC(F)(F)c1ccccc1)c1nnnn1CCOC(=O)NCCCCO
CHEMBL4640507 ghsr_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL1162065 ghsr_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
655 12 5 5 4.1 NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)c1ccccc1
CHEMBL1162065 ghsr_human Human No 9.6 EC50 = 0.3 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
655 12 5 5 4.1 NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1)c1ccccc1
CHEMBL270666 ghsr_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1O
CHEMBL4647963 ghsr_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL482220 ghsr_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
481 4 1 4 3.8 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3cc(Cl)ccc3Cl)cc2)C1
CHEMBL2364468 ghsr_human Human No 9.5 EC50 = 0.3 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1Cl
CHEMBL4647963 ghsr_human Human No 9.5 EC50 = 0.3 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL322912 ghsr_human Human No 9.5 EC50 = 0.3 nM Funct
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
683 14 4 5 4.3 NC(=O)CN(CCc1ccccc1)C(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1
CHEMBL539929 ghsr_human Human No 9.5 EC50 = 0.3 nM Funct
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
539 15 4 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1-c1ccccc1)c1nnnn1CCOC(=O)NCCCCO
CHEMBL13817 ghsr_human Human Yes 9.4 EC50 = 0.4 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C
CHEMBL4639111 ghsr_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4639229 ghsr_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL260819 ghsr_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
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
CHEMBL519301 ghsr_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
421 4 1 5 2.1 Cc1ccc(-c2ccc(S(=O)(=O)N3CCC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1
CHEMBL2364427 ghsr_human Human No 9.4 EC50 = 0.4 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
485 6 2 6 5.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)cc1C
CHEMBL13817 ghsr_human Human Yes 9.4 EC50 = 0.4 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C
CHEMBL271876 ghsr_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccn1
CHEMBL404545 ghsr_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@H](CC#N)COc1ccccc1
CHEMBL254765 ghsr_human Human No 9.4 EC50 = 0.4 nM Funct
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
499 14 4 10 0.6 CC(C)(N)C(=O)N[C@H](COCc1ccc(F)cc1F)c1nnnn1CCOC(=O)NCCCCO
CHEMBL4639111 ghsr_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4639229 ghsr_human Human No 9.4 EC50 = 0.4 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL428592 ghsr_human Human No 9.4 EC50 = 0.5 nM Funct
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
497 14 4 10 0.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1Cl)c1nnnn1CCOC(=O)NCCCCO
CHEMBL4646219 ghsr_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL179823 ghsr_human Human No 9.3 EC50 = 0.5 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
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
CHEMBL180094 ghsr_human Human No 9.3 EC50 = 0.5 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C
CHEMBL180094 ghsr_human Human No 9.3 EC50 = 0.5 nM Funct
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C
CHEMBL180094 ghsr_human Human No 9.3 EC50 = 0.5 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
495 8 1 5 5.5 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C
CHEMBL360547 ghsr_human Human No 9.3 EC50 = 0.5 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
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
CHEMBL360547 ghsr_human Human No 9.3 EC50 = 0.5 nM Funct
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
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
CHEMBL404336 ghsr_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(/C=C/c1ccccc1)CC#N
CHEMBL251169 ghsr_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
451 4 1 5 3.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc3ccccc3c1)CC2
CHEMBL4636502 ghsr_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4646219 ghsr_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL272753 ghsr_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
503 6 2 5 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(Cl)ccc2F)cc1
CHEMBL480037 ghsr_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
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
CHEMBL2364429 ghsr_human Human No 9.3 EC50 = 0.5 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)cc1F
CHEMBL2364472 ghsr_human Human No 9.3 EC50 = 0.5 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
475 6 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1Cl
CHEMBL404354 ghsr_human Human No 9.3 EC50 = 0.5 nM Funct
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
477 14 4 10 0.6 Cc1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO
CHEMBL4636502 ghsr_human Human No 9.3 EC50 = 0.5 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL1161835 ghsr_human Human No 9.2 EC50 = 0.6 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
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
CHEMBL2413152 ghsr_human Human No 9.2 EC50 = 0.6 nM Bind
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
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
CHEMBL411259 ghsr_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
489 17 4 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCCCO
CHEMBL256235 ghsr_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
481 12 2 9 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)COc1ccccc1F
CHEMBL1161835 ghsr_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
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
CHEMBL2113324 ghsr_human Human No 9.2 EC50 = 0.6 nM Funct
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
631 12 4 7 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)c(OC)c1
CHEMBL1161835 ghsr_human Human No 9.2 EC50 = 0.6 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
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
CHEMBL1161835 ghsr_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
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
CHEMBL401827 ghsr_human Human No 9.2 EC50 = 0.6 nM Funct
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
531 14 4 10 1.6 CC(C)(N)C(=O)N[C@H](COCc1cccc(Cl)c1Cl)c1nnnn1CCOC(=O)NCCCCO
CHEMBL2364354 ghsr_human Human No 9.2 EC50 = 0.6 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
472 6 2 7 4.1 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)n3)s2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL410135 ghsr_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
495 13 4 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCNC(=O)CCc1cccc(O)c1
CHEMBL369329 ghsr_human Human No 9.2 EC50 = 0.7 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
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
CHEMBL411697 ghsr_human Human No 9.2 EC50 = 0.7 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
477 16 4 10 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCOCCO
CHEMBL254973 ghsr_human Human No 9.1 EC50 = 0.7 nM Funct
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
531 14 4 10 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1C(F)(F)F)c1nnnn1CCOC(=O)NCCCCO
CHEMBL178900 ghsr_human Human No 9.1 EC50 = 0.7 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
529 8 1 5 6.2 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccc(Cl)cc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C
CHEMBL4647797 ghsr_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL2304221 ghsr_human Human No 9.1 EC50 = 0.8 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
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
CHEMBL379074 ghsr_human Human No 9.1 EC50 = 0.8 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1
CHEMBL248544 ghsr_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
498 5 1 7 4.1 COc1cc2c(cc1N1C[C@H](C)NC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2
CHEMBL310457 ghsr_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
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
CHEMBL379074 ghsr_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1
CHEMBL4637980 ghsr_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4647797 ghsr_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL272993 ghsr_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1Cl
CHEMBL407706 ghsr_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1
CHEMBL407706 ghsr_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cc1
CHEMBL2364408 ghsr_human Human No 9.1 EC50 = 0.8 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
477 6 2 7 4.8 COc1ccc(NS(=O)(=O)c2ccc(-c3cc(C)cs3)s2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2304221 ghsr_human Human No 9.1 EC50 = 0.8 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
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
CHEMBL379074 ghsr_human Human No 9.1 EC50 = 0.8 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1
CHEMBL403180 ghsr_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1
CHEMBL310457 ghsr_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
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
CHEMBL379074 ghsr_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
491 11 1 4 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1cccs1
CHEMBL3798559 ghsr_human Human No 9.1 EC50 = 0.8 nM Funct
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
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
CHEMBL4649634 ghsr_human Human No 9.1 EC50 = 0.8 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4637980 ghsr_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL179785 ghsr_human Human No 9.1 EC50 = 0.9 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
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
CHEMBL471751 ghsr_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at GHS receptorAgonist activity at GHS receptor
391 9 2 7 2.1 CC(C)(N)C(=O)N[C@H](CCC(F)(F)c1ccccc1)c1nnnn1CCC#N
CHEMBL113313 ghsr_human Human Yes 9.1 EC50 = 0.9 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
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
CHEMBL262358 ghsr_human Human No 9.1 EC50 = 0.9 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
539 16 4 10 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1ccccc1C(=O)NCCCCO
CHEMBL113313 ghsr_human Human Yes 9.0 EC50 = 0.9 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
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
CHEMBL4647258 ghsr_human Human No 9.0 EC50 = 0.9 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL47938 ghsr_human Human Yes 9.0 EC50 = 1 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
513 7 4 4 3.5 CNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1
CHEMBL1162063 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
534 11 4 6 2.6 NCC(O)CNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCCN1C(=O)CCSc2ccccc21
CHEMBL47938 ghsr_human Human Yes 9.0 EC50 = 1 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
513 7 4 4 3.5 CNC(=O)NCc1ccccc1-c1ccc(CN2C(=O)[C@H](NC(=O)C(C)(C)N)CCc3ccccc32)cc1
CHEMBL4645148 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4647258 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4649603 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4649634 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL1923504 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
494 4 3 5 2.1 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O
CHEMBL1923512 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
510 4 4 6 1.8 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CN(C)C1=O
CHEMBL1923609 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL1923610 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C
CHEMBL1923617 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL1923626 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL1923638 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL1923642 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL1923502 ghsr_human Human Yes 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL1963249 ghsr_human Human Yes 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3889512 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3893048 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3895776 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3898348 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
552 2 4 5 3.4 CC1(C)NC(=O)C2(CCCC2)NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2cccc(Cl)c2)NC1=O
CHEMBL3898794 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3900284 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3903845 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
533 4 4 5 2.6 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CN(C)C1=O
CHEMBL3905791 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3907497 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3909834 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3910300 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3913052 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3913335 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
534 3 4 6 1.8 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOC2)NC1=O
CHEMBL3913855 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3915269 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3916659 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3918046 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3920049 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3921499 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3922056 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3922810 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3927481 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3932408 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3932434 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
544 2 4 5 3.3 O=C1NC/C=C\c2ccccc2OCCNC2(CCCC2)C(=O)NC2(CCCC2)C(=O)N[C@H]1Cc1ccccc1
CHEMBL3934402 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3937200 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3938104 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3940705 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3943086 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3946348 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3958460 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3959108 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3970499 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3973085 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL517543 ghsr_human Human No 9.0 EC50 = 1 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
449 4 1 4 2.7 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3cc(F)ccc3F)cc2)C1
CHEMBL237699 ghsr_human Human No 9.0 EC50 = 1 nM Funct
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
461 10 3 10 -0.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)N1CC[C@@H](O)C1
CHEMBL2364338 ghsr_human Human No 9.0 EC50 = 1 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
444 5 2 6 3.8 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cccc(N4C[C@H](C)N[C@H](C)C4)n3)cc2F)o1
CHEMBL2364353 ghsr_human Human No 9.0 EC50 = 1 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364382 ghsr_human Human No 9.0 EC50 = 1 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccc3)s2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364403 ghsr_human Human No 9.0 EC50 = 1 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2C)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL414394 ghsr_human Human No 9.0 EC50 = 1.0 nM Funct
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
558 15 4 12 1.6 Cc1noc(C)c1-c1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO
CHEMBL4645148 ghsr_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4649603 ghsr_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL1161828 ghsr_human Human No 9.0 EC50 = 1.1 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12
CHEMBL1161828 ghsr_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12
CHEMBL1161828 ghsr_human Human No 9.0 EC50 = 1.1 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12
CHEMBL1161828 ghsr_human Human No 9.0 EC50 = 1.1 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
497 7 2 5 2.6 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12
CHEMBL254565 ghsr_human Human No 9.0 EC50 = 1.1 nM Funct
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
493 15 4 11 0.3 COc1ccccc1COC[C@@H](NC(=O)C(C)(C)N)c1nnnn1CCOC(=O)NCCCCO
CHEMBL404355 ghsr_human Human No 8.9 EC50 = 1.2 nM Funct
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
540 15 4 11 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1-c1cccnc1)c1nnnn1CCOC(=O)NCCCCO
CHEMBL13675 ghsr_rat Rat No 8.9 EC50 = 1.2 nM Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
490 5 4 5 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CC(O)c3ccccc3O2)C1
CHEMBL275093 ghsr_rat Rat No 8.9 EC50 = 1.2 nM Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
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
CHEMBL4170481 ghsr_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
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
CHEMBL516602 ghsr_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
418 4 2 6 0.8 Cc1ccc(-c2ccc(S(=O)(=O)N3CCNC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2)o1
CHEMBL2364424 ghsr_human Human No 8.9 EC50 = 1.3 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
455 5 2 5 5.0 Cc1csc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3C)cc2)c1
CHEMBL2364432 ghsr_human Human No 8.9 EC50 = 1.3 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cc(C)cs3)cc2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL254363 ghsr_human Human No 8.9 EC50 = 1.3 nM Funct
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
488 14 4 11 0.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1C#N)c1nnnn1CCOC(=O)NCCCCO
CHEMBL209360 ghsr_human Human No 8.9 EC50 = 1.3 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
465 7 3 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12
CHEMBL4765101 ghsr_rat Rat No 8.9 EC50 = 1.3 nM Bind
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
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
CHEMBL3218890 ghsr_human Human No 8.9 EC50 = 1.3 nM Bind
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
472 6 0 8 4.1 COc1cccc(-n2cc3nc(-c4cccnc4C)n(C[C@H]4CCCN(C(C)C)C4)c(=O)c3n2)c1
CHEMBL261358 ghsr_human Human No 8.9 EC50 = 1.3 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
475 16 4 9 0.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCCO
CHEMBL13817 ghsr_human Human Yes 8.9 EC50 = 1.3 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C
CHEMBL13817 ghsr_rat Rat Yes 8.9 EC50 = 1.3 nM Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C
CHEMBL209360 ghsr_human Human No 8.9 EC50 = 1.3 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
465 7 3 5 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)C[C@@H](O)c1ccccc12
CHEMBL13817 ghsr_human Human Yes 8.9 EC50 = 1.3 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C
CHEMBL4170481 ghsr_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
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
CHEMBL258761 ghsr_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
496 14 4 10 -1.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCS(N)(=O)=O
CHEMBL500468 ghsr_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
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
CHEMBL500468 ghsr_human Human No 8.9 EC50 = 1.4 nM Funct
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
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
CHEMBL180246 ghsr_human Human No 8.9 EC50 = 1.4 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
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
CHEMBL500468 ghsr_human Human No 8.9 EC50 = 1.4 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
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
CHEMBL4753794 ghsr_human Human No 8.9 EC50 = 1.4 nM Funct
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
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
CHEMBL500468 ghsr_human Human No 8.9 EC50 = 1.4 nM Funct
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
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
CHEMBL500468 ghsr_human Human No 8.9 EC50 = 1.4 nM Funct
Agonist activity at GHS receptorAgonist activity at GHS receptor
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
CHEMBL13817 ghsr_human Human Yes 8.9 EC50 = 1.4 nM Funct
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
528 8 2 6 1.8 O=C([C@H](NC(=O)C(N)(C)C)COCc1ccccc1)N1CCC2(CC1)CN(c1c2cccc1)S(=O)(=O)C
CHEMBL4636571 ghsr_human Human No 8.8 EC50 = 1.5 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL181063 ghsr_human Human No 8.8 EC50 = 1.5 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
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
CHEMBL181764 ghsr_human Human No 8.8 EC50 = 1.5 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
553 11 1 7 4.5 COC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C
CHEMBL181764 ghsr_human Human No 8.8 EC50 = 1.5 nM Funct
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
553 11 1 7 4.5 COC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C
CHEMBL122939 ghsr_rat Rat No 8.8 EC50 = 1.5 nM Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
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
CHEMBL425281 ghsr_human Human Yes 8.8 EC50 = 1.5 nM Funct
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
3369 117 48 48 -14.9 CCCCCCCC(=O)OC[C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC3=CNC=N3)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCC(=O)N)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)N4CCC[C@H]4C(=O)N5CCC[C@H]5C(=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(=O)N)C(=O)N6CCC[C@H]6C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)NC(=O)[C@H](CO)NC(=O)CN
CHEMBL433087 ghsr_human Human No 8.8 EC50 = 1.6 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
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
CHEMBL4164328 ghsr_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1
CHEMBL79263 ghsr_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
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
CHEMBL4636571 ghsr_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4639379 ghsr_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1
CHEMBL2364381 ghsr_human Human No 8.8 EC50 = 1.6 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
463 6 2 7 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3ccsc3)s2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364384 ghsr_human Human No 8.8 EC50 = 1.6 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
459 5 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc2c(Cl)cccc2c1
CHEMBL2364426 ghsr_human Human No 8.8 EC50 = 1.6 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
477 6 2 7 4.8 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(C)s3)s2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364430 ghsr_human Human No 8.8 EC50 = 1.6 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
459 6 2 6 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1F
CHEMBL2364475 ghsr_human Human No 8.8 EC50 = 1.6 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
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
CHEMBL433087 ghsr_human Human No 8.8 EC50 = 1.6 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
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
CHEMBL266063 ghsr_human Human No 8.8 EC50 = 1.6 nM Funct
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
601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1
CHEMBL79263 ghsr_human Human No 8.8 EC50 = 1.6 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
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
CHEMBL240509 ghsr_human Human No 8.8 EC50 = 1.6 nM Funct
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
564 11 4 6 4.6 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)cc1
CHEMBL254766 ghsr_human Human No 8.8 EC50 = 1.6 nM Funct
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
497 14 4 10 0.9 CC(C)(N)C(=O)N[C@H](COCc1cccc(Cl)c1)c1nnnn1CCOC(=O)NCCCCO
CHEMBL254566 ghsr_human Human No 8.8 EC50 = 1.7 nM Funct
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
469 14 4 10 0.7 CC(C)(N)C(=O)N[C@H](COCC1CCCCC1)c1nnnn1CCOC(=O)NCCCCO
CHEMBL105462 ghsr_rat Rat Yes 8.8 EC50 = 1.7 nM Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
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
CHEMBL253965 ghsr_human Human No 8.8 EC50 = 1.8 nM Funct
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
531 14 4 10 1.3 CC(C)(N)C(=O)N[C@H](COCc1cccc(C(F)(F)F)c1)c1nnnn1CCOC(=O)NCCCCO
CHEMBL261544 ghsr_human Human No 8.7 EC50 = 1.8 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
461 15 4 9 0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCCO
CHEMBL133848 ghsr_human Human No 8.7 EC50 = 1.8 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
509 9 4 4 3.7 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1ccc2ccccc2c1)C1CCNCC1
CHEMBL13687 ghsr_rat Rat No 8.7 EC50 = 1.8 nM Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
488 5 3 5 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CC(=O)c3ccccc3O2)C1
CHEMBL331093 ghsr_rat Rat No 8.7 EC50 = 1.8 nM Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
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
CHEMBL133848 ghsr_human Human No 8.7 EC50 = 1.8 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
509 9 4 4 3.7 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1ccc2ccccc2c1)C1CCNCC1
CHEMBL4632657 ghsr_human Human No 8.7 EC50 = 1.9 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL398372 ghsr_human Human Yes 8.7 EC50 = 1.9 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO
CHEMBL398372 ghsr_human Human Yes 8.7 EC50 = 1.9 nM Funct
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
463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO
CHEMBL398372 ghsr_human Human Yes 8.7 EC50 = 1.9 nM Funct
Agonist activity at GHS receptorAgonist activity at GHS receptor
463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO
CHEMBL398372 ghsr_human Human Yes 8.7 EC50 = 1.9 nM Funct
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
463 14 4 10 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCO
CHEMBL295984 ghsr_human Human No 8.7 EC50 = 2.0 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O
CHEMBL1162063 ghsr_human Human No 8.7 EC50 = 2.0 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
534 11 4 6 2.6 NCC(O)CNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCCN1C(=O)CCSc2ccccc21
CHEMBL295984 ghsr_human Human No 8.7 EC50 = 2.0 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O
CHEMBL4632657 ghsr_human Human No 8.7 EC50 = 2.0 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4637284 ghsr_human Human No 8.7 EC50 = 2.0 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4640615 ghsr_human Human No 8.7 EC50 = 2.0 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL261030 ghsr_human Human No 8.7 EC50 = 2.0 nM Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
481 7 2 6 4.4 COc1cccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)cc2)c1
CHEMBL270790 ghsr_human Human No 8.7 EC50 = 2.0 nM Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
475 6 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1F
CHEMBL481620 ghsr_human Human No 8.7 EC50 = 2.0 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
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
CHEMBL2364399 ghsr_human Human No 8.7 EC50 = 2.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
463 6 2 7 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)s2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364407 ghsr_human Human No 8.7 EC50 = 2.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
477 6 2 7 4.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)s1
CHEMBL2364441 ghsr_human Human No 8.7 EC50 = 2.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
455 6 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1C
CHEMBL2364480 ghsr_human Human No 8.7 EC50 = 2.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
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
CHEMBL1161825 ghsr_human Human No 8.0 EC50 = 10 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
467 7 2 5 3.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12
CHEMBL294923 ghsr_human Human No 8.0 EC50 = 10 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL540001 ghsr_human Human No 8.0 EC50 = 10 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL488965 ghsr_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
406 7 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(Cc1cccc(Cl)c1)C[C@H]1CCCN1
CHEMBL248745 ghsr_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
498 5 1 7 4.1 COc1cc2c(cc1N1C[C@@H](C)NC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2
CHEMBL4160705 ghsr_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
446 4 2 5 2.4 CN1CCCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1
CHEMBL4171914 ghsr_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21
CHEMBL237926 ghsr_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
523 15 3 9 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCCCNC(=O)OCc1ccccc1
CHEMBL106841 ghsr_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
498 9 5 4 3.1 O=C(N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CO)Cc1c[nH]c2ccccc12)C1CCNCC1
CHEMBL1161825 ghsr_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
467 7 2 5 3.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CC1)CSc1ccccc12
CHEMBL1162062 ghsr_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
522 9 3 6 1.5 NCCNC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)CCN1C(=O)CCS(=O)(=O)c2ccccc21
CHEMBL294923 ghsr_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL540001 ghsr_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
447 7 2 3 3.7 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL3798645 ghsr_human Human No 8.0 EC50 = 10 nM Funct
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
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
CHEMBL4637255 ghsr_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4641201 ghsr_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL256808 ghsr_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1
CHEMBL482203 ghsr_human Human No 8.0 EC50 = 10 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
431 5 1 5 2.6 CNC1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccc(C)o3)cc2)C1
CHEMBL105462 ghsr_rat Rat Yes 8.0 EC50 = 10 nM Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
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
CHEMBL2364343 ghsr_human Human No 8.0 EC50 = 10 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
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
CHEMBL2364358 ghsr_human Human No 8.0 EC50 = 10 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
466 6 2 6 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)cc1
CHEMBL2364359 ghsr_human Human No 8.0 EC50 = 10 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
472 6 2 7 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(C)n2)s1
CHEMBL2364377 ghsr_human Human No 8.0 EC50 = 10 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
431 5 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1csc2ccccc12
CHEMBL2364390 ghsr_human Human No 8.0 EC50 = 10 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
395 4 2 4 3.8 C[C@H]1CN(c2cccc(NS(=O)(=O)c3cccc4ccccc34)c2)C[C@@H](C)N1
CHEMBL2364431 ghsr_human Human No 8.0 EC50 = 10 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
459 5 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc2cccc(Cl)c12
CHEMBL2364444 ghsr_human Human No 8.0 EC50 = 10 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
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
CHEMBL2364477 ghsr_human Human No 8.0 EC50 = 10 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
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
CHEMBL2364479 ghsr_human Human No 8.0 EC50 = 10 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
472 6 2 7 4.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cc(C)cs2)nc1
CHEMBL393531 ghsr_human Human No 8.0 EC50 = 10.1 nM Funct
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
475 10 3 10 0.4 CC1(O)CCN(C(=O)OCCn2nnnc2[C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)C1
CHEMBL4641201 ghsr_human Human No 8.0 EC50 = 10.2 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4294083 ghsr_human Human No 8.0 EC50 = 10.6 nM Funct
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
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
CHEMBL4637255 ghsr_human Human No 8.0 EC50 = 10.8 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL473921 ghsr_human Human No 7.0 EC50 = 100 nM Bind
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1
CHEMBL4174476 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1
CHEMBL442151 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
436 8 2 4 2.9 Cc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1
CHEMBL263916 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
486 7 2 7 4.6 CC(C)Oc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1
CHEMBL271948 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
481 8 2 6 4.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(OCc2ccccc2)cc1
CHEMBL410013 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
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
CHEMBL1923628 ghsr_human Human No 7.0 EC50 = 100 nM Funct
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
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
CHEMBL1923631 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL1923634 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL1923636 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL1923637 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3890296 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O
CHEMBL3896536 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3905987 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
534 3 4 5 2.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O
CHEMBL3908264 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3910661 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
548 3 4 6 2.2 CC(C)[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCOCC2)NC1=O
CHEMBL3914338 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
472 4 3 4 3.0 CCC(C)C1NCCCCCCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O
CHEMBL3924192 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3937924 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
520 4 4 5 2.5 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CC2)NC1=O
CHEMBL3940653 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
548 4 4 5 3.3 CC(C)C[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@H](Cc2ccccc2)NC(=O)C2(CCCC2)NC1=O
CHEMBL3942642 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3958451 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3961108 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3963078 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3967506 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
506 4 3 4 3.2 CCC(C)C1NCc2ccccc2CCCCNC(=O)C(Cc2ccccc2)NC(=O)C(C)N(C)C1=O
CHEMBL3967783 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3970180 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3973940 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL3978207 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C\CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O
CHEMBL3981072 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
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
CHEMBL473921 ghsr_human Human No 7.0 EC50 = 100 nM Funct
Agonist activity at human Ghrelin receptorAgonist activity at human Ghrelin receptor
501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1
CHEMBL473921 ghsr_human Human No 7.0 EC50 = 100 nM Bind
Inhibition of human Ghrelin receptorInhibition of human Ghrelin receptor
501 6 2 5 4.8 C[C@H]1CN(Cc2ccc(-c3cccnc3C(=O)N3CCC(Nc4ccc(F)cc4)CC3)cc2)C[C@@H](C)N1
CHEMBL506986 ghsr_human Human No 7.0 EC50 = 100 nM Funct
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
891 25 10 8 3.1 CC(C)C[C@@H](C(=O)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1=CNC2=CC=CC=C21)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@@H](CC4=CNC5=CC=CC=C54)NC(=O)[C@H](CCCCN)N
CHEMBL3578015 ghsr_human Human No 7.0 EC50 = 100 nM Funct
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
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
CHEMBL3578018 ghsr_human Human No 7.0 EC50 = 100 nM Funct
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
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
CHEMBL2364364 ghsr_human Human No 7.0 EC50 = 100 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
452 6 2 6 3.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccnc2)cc1
CHEMBL2364366 ghsr_human Human No 7.0 EC50 = 100 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccnc2)s1
CHEMBL2364375 ghsr_human Human No 7.0 EC50 = 100 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
452 5 2 6 4.3 C[C@H]1CN(c2cc(NS(=O)(=O)c3ccc(-c4cccs4)cc3)ccc2C#N)C[C@@H](C)N1
CHEMBL2364376 ghsr_human Human No 7.0 EC50 = 100 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
497 8 2 7 4.5 COc1ccc(Oc2cccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3OC)c2)cc1
CHEMBL2364397 ghsr_human Human No 7.0 EC50 = 100 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
465 6 2 5 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccc3C)cc2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364414 ghsr_human Human No 7.0 EC50 = 100 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(F)cc3)s2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364418 ghsr_human Human No 7.0 EC50 = 100 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
437 4 2 4 3.7 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)cc1
CHEMBL2364434 ghsr_human Human No 7.0 EC50 = 100 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
487 6 2 5 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(F)cc2F)cc1
CHEMBL2364463 ghsr_human Human No 7.0 EC50 = 100 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
471 5 2 5 3.6 COc1cc(Br)ccc1S(=O)(=O)Nc1cc(N2C[C@H](C)N[C@H](C)C2)ccc1F
CHEMBL519171 ghsr_human Human No 6.0 EC50 = 1000 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
381 7 2 4 3.2 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1
CHEMBL4647751 ghsr_human Human No 6.0 EC50 = 1000 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL3918783 ghsr_human Human No 7.0 EC50 = 104 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
508 5 3 5 2.5 CCCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O
CHEMBL261497 ghsr_human Human No 7.0 EC50 = 105 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
601 17 4 11 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1cccc(S(=O)(=O)CCO)c1
CHEMBL4647751 ghsr_human Human No 6.0 EC50 = 1050 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL235135 ghsr_human Human No 7.0 EC50 = 107 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
515 13 3 9 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCCc2ccccc2NS(C)(=O)=O)n1
CHEMBL3578018 ghsr_human Human No 7.0 EC50 = 109.6 nM Funct
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
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
CHEMBL258550 ghsr_human Human No 8.0 EC50 = 11 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
511 14 4 10 0.6 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1ccccc1C(=O)NCCO
CHEMBL374992 ghsr_human Human No 8.0 EC50 = 11 nM Funct
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
534 11 3 5 5.3 CCc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1
CHEMBL1923626 ghsr_human Human No 8.0 EC50 = 11 nM Funct
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
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
CHEMBL2170781 ghsr_human Human Yes 8.0 EC50 = 11.2 nM Funct
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
902 25 9 8 3.8 CC(C)C[C@@H](C(=O)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1=CNC2=CC=CC=C21)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@@H](CC4=CC=CC5=CC=CC=C54)NC(=O)[C@H](CCCCN)N
CHEMBL181092 ghsr_human Human No 7.9 EC50 = 11.7 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
509 9 1 5 5.3 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C
CHEMBL237058 ghsr_human Human No 6.0 EC50 = 1120 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
394 9 2 7 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(Cc2ccccc2)n1
CHEMBL392522 ghsr_human Human No 6.9 EC50 = 116 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1cccc(NS(C)(=O)=O)c1
CHEMBL4292914 ghsr_human Human No 6.9 EC50 = 117 nM Funct
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
523 4 1 2 6.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(C#CC3CC3)c(Cl)c2Cl)CC1
CHEMBL2170775 ghsr_human Human No 6.9 EC50 = 119.6 nM Funct
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
None None None CC(C)C[C@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
CHEMBL238155 ghsr_human Human No 7.9 EC50 = 12 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
420 10 2 7 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C/C=C/c1ccccc1
CHEMBL240522 ghsr_human Human No 7.9 EC50 = 12 nM Funct
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
565 11 5 7 3.1 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1
CHEMBL385131 ghsr_human Human No 7.9 EC50 = 12 nM Funct
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
534 11 3 5 5.4 Cc1ccc(Cn2c(CCCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)cc1
CHEMBL252643 ghsr_human Human No 7.9 EC50 = 12 nM Funct
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
595 11 3 6 6.2 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)cc1
CHEMBL181108 ghsr_human Human No 7.9 EC50 = 12 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
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
CHEMBL2170781 ghsr_human Human Yes 7.9 EC50 = 12 nM Funct
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
902 25 9 8 3.8 CC(C)C[C@@H](C(=O)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1=CNC2=CC=CC=C21)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@@H](CC4=CC=CC5=CC=CC=C54)NC(=O)[C@H](CCCCN)N
CHEMBL4643595 ghsr_human Human No 7.9 EC50 = 12.4 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4174302 ghsr_human Human No 7.9 EC50 = 12.6 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1
CHEMBL4635743 ghsr_human Human No 7.9 EC50 = 12.6 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4643595 ghsr_human Human No 7.9 EC50 = 12.6 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL2364336 ghsr_human Human No 7.9 EC50 = 12.6 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(Cl)s2)cc1
CHEMBL2364387 ghsr_human Human No 7.9 EC50 = 12.6 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
471 7 2 6 4.8 CCOc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1
CHEMBL2364419 ghsr_human Human No 7.9 EC50 = 12.6 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
447 6 2 7 4.0 COc1ccc(NS(=O)(=O)c2ccc(-c3ccoc3)s2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364433 ghsr_human Human No 7.9 EC50 = 12.6 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
441 6 2 6 3.9 COc1ccc(NS(=O)(=O)c2ccc(-c3ccoc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364451 ghsr_human Human No 7.9 EC50 = 12.6 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
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
CHEMBL2364458 ghsr_human Human No 7.9 EC50 = 12.6 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
458 6 2 7 3.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2nccs2)cc1
CHEMBL2364483 ghsr_human Human No 7.9 EC50 = 12.6 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
453 6 2 7 3.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ncccn2)cc1
CHEMBL2364486 ghsr_human Human No 7.9 EC50 = 12.6 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
471 6 1 6 4.8 COc1ccc(N2C[C@H](C)N(C)[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1
CHEMBL2170779 ghsr_human Human No 7.9 EC50 = 12.6 nM Funct
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
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
CHEMBL482623 ghsr_human Human No 6.9 EC50 = 120 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
386 7 1 3 4.2 Cc1cccc(CN(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)c1
CHEMBL489403 ghsr_human Human No 6.9 EC50 = 120 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
392 6 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1ccc(Cl)cc1
CHEMBL528332 ghsr_human Human No 6.9 EC50 = 120 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
358 6 1 3 3.9 CC(Oc1cccc(Cl)c1)C(=O)N(C[C@H]1CCCN1)c1ccccc1
CHEMBL521612 ghsr_human Human No 5.9 EC50 = 1200 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)[C@@H](C)Oc2cccc(Cl)c2)cc1
CHEMBL4283504 ghsr_human Human No 6.9 EC50 = 121 nM Funct
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
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
CHEMBL4642860 ghsr_human Human No 5.9 EC50 = 1220 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL2170776 ghsr_human Human No 6.9 EC50 = 124.1 nM Funct
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
None None 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
CHEMBL501315 ghsr_rabit Rabbit No 6.9 EC50 = 125.9 nM Funct
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
568 10 2 4 6.6 COc1cccc(CCN(Cc2ccccc2-c2ccc(CN3C[C@H](C)N[C@H](C)C3)cc2)C(=O)NC2CCCCC2)c1
CHEMBL501315 ghsr_human Human No 6.9 EC50 = 125.9 nM Bind
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
568 10 2 4 6.6 COc1cccc(CCN(Cc2ccccc2-c2ccc(CN3C[C@H](C)N[C@H](C)C3)cc2)C(=O)NC2CCCCC2)c1
CHEMBL399704 ghsr_human Human No 6.9 EC50 = 125.9 nM Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
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
CHEMBL4160261 ghsr_human Human No 6.9 EC50 = 125.9 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)c(F)cc21
CHEMBL4167776 ghsr_human Human No 6.9 EC50 = 125.9 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
432 4 4 4 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCOC3)cc2c1
CHEMBL4171137 ghsr_human Human No 6.9 EC50 = 125.9 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1
CHEMBL4635694 ghsr_human Human No 6.9 EC50 = 125.9 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
599 7 2 7 2.5 CC(=O)N1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1
CHEMBL261466 ghsr_human Human No 6.9 EC50 = 125.9 nM Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
453 5 2 5 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)cc1
CHEMBL2364349 ghsr_human Human No 6.9 EC50 = 125.9 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
467 7 2 6 4.5 COc1ccc(NS(=O)(=O)c2ccc(Oc3ccccc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364357 ghsr_human Human No 6.9 EC50 = 125.9 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
459 5 2 6 3.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(Br)s1
CHEMBL4642860 ghsr_human Human No 5.9 EC50 = 1258.9 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL485091 ghsr_human Human No 5.9 EC50 = 1260 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
358 6 1 3 3.9 CC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccccc1Cl
CHEMBL4291926 ghsr_human Human No 5.9 EC50 = 1276 nM Funct
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
601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1
CHEMBL4171137 ghsr_human Human No 6.9 EC50 = 129 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
416 4 2 4 2.6 CN1CC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1
CHEMBL330860 ghsr_rat Rat No 7.9 EC50 = 13 nM Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
542 12 2 4 4.1 CCNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N
CHEMBL181627 ghsr_human Human No 7.9 EC50 = 13.1 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
555 13 1 4 5.9 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CCCc1ccccc1)C(C)C
CHEMBL2170783 ghsr_human Human No 7.9 EC50 = 13.1 nM Funct
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
None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](NC(=O)[C@@H](N)CCCCN)C(c1ccccc1)c1ccccc1)C(N)=O
CHEMBL2170779 ghsr_human Human No 7.9 EC50 = 13.4 nM Funct
Agonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
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
CHEMBL4635743 ghsr_human Human No 7.9 EC50 = 13.9 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4635694 ghsr_human Human No 6.9 EC50 = 132.5 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
599 7 2 7 2.5 CC(=O)N1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1
CHEMBL1923501 ghsr_human Human No 6.9 EC50 = 134 nM Funct
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
492 4 3 5 2.2 CCC[C@@H]1NCCOc2ccccc2/C=C/CNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O
CHEMBL3934561 ghsr_human Human No 6.9 EC50 = 134 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
494 3 3 5 1.9 CC(C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(C)C1=O
CHEMBL4456830 ghsr_human Human No 6.9 EC50 = 134 nM Funct
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
1174 34 16 14 -2.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)[C@@H](C)O
CHEMBL4160261 ghsr_human Human No 6.9 EC50 = 135 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
443 4 3 5 3.1 Cn1ccc2cc(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)c(F)cc21
CHEMBL4167776 ghsr_human Human No 6.9 EC50 = 137 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
432 4 4 4 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@@H]3CNCCOC3)cc2c1
CHEMBL403180 ghsr_human Human No 6.9 EC50 = 139 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1C(CC#N)CCc1ccccc1
CHEMBL274599 ghsr_human Human No 7.9 EC50 = 14 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL558802 ghsr_human Human No 7.9 EC50 = 14 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL1923617 ghsr_human Human No 7.9 EC50 = 14 nM Funct
Agonist activity at ghrelin receptor by cell based assayAgonist activity at ghrelin receptor by cell based assay
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
CHEMBL4174302 ghsr_human Human No 7.9 EC50 = 14 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
425 4 4 4 3.3 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)cc2c1
CHEMBL392076 ghsr_human Human No 7.9 EC50 = 14 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
529 13 2 9 1.8 CN(c1ccccc1CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N)S(C)(=O)=O
CHEMBL274599 ghsr_human Human No 7.9 EC50 = 14 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL558802 ghsr_human Human No 7.9 EC50 = 14 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL392663 ghsr_human Human No 7.9 EC50 = 14 nM Funct
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
580 11 4 7 4.6 COc1ccc(N2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CCNCC3)=NNC2CCc2ccccc2)c(OC)c1
CHEMBL274599 ghsr_rat Rat No 7.9 EC50 = 14 nM Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL558802 ghsr_rat Rat No 7.9 EC50 = 14 nM Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL274599 ghsr_human Human No 7.9 EC50 = 14.1 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL558802 ghsr_human Human No 7.9 EC50 = 14.1 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL274599 ghsr_human Human No 7.9 EC50 = 14.1 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL558802 ghsr_human Human No 7.9 EC50 = 14.1 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
458 5 3 3 3.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL442151 ghsr_human Human No 7.9 EC50 = 14.1 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
436 8 2 4 2.9 Cc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1
CHEMBL4793824 ghsr_human Human No 7.9 EC50 = 14.2 nM Funct
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
681 14 3 7 5.9 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(F)cc2)cc1
CHEMBL181247 ghsr_human Human No 7.8 EC50 = 14.4 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
508 9 2 4 4.9 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)NC(C)(C)C)C(C)C
CHEMBL393330 ghsr_human Human No 7.8 EC50 = 14.6 nM Funct
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
477 15 4 10 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCCCCO
CHEMBL411122 ghsr_human Human No 7.8 EC50 = 14.7 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
481 13 3 10 -0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCNC(=O)CCS(C)(=O)=O
CHEMBL483455 ghsr_human Human No 6.9 EC50 = 140 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1ccccc1Cl
CHEMBL490627 ghsr_human Human No 6.9 EC50 = 140 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
415 7 2 4 3.9 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)c1
CHEMBL263141 ghsr_human Human No 6.9 EC50 = 140 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
489 15 3 10 0.6 CCOC(=O)CCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N
CHEMBL375102 ghsr_human Human No 6.9 EC50 = 140 nM Funct
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
612 12 5 5 6.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1c[nH]c2ccccc12
CHEMBL490390 ghsr_human Human No 4.9 EC50 = 14000 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
377 8 1 4 3.7 CCC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1ccc(CC#N)cc1
CHEMBL239464 ghsr_human Human No 6.8 EC50 = 143 nM Funct
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
563 11 5 6 3.7 CCc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)cc1
CHEMBL237717 ghsr_human Human No 6.8 EC50 = 147 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
513 10 2 9 1.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC1CN(S(C)(=O)=O)c2ccccc21
CHEMBL4167481 ghsr_human Human No 7.8 EC50 = 15 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21
CHEMBL2113327 ghsr_human Human No 7.8 EC50 = 15 nM Funct
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
585 10 4 5 6.0 CCc1ccc(-n2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1
CHEMBL223725 ghsr_human Human No 7.8 EC50 = 15 nM Funct
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
573 12 4 5 5.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCCc2c[nH]c3ccccc23)n1CCc1ccccc1
CHEMBL4759418 ghsr_human Human No 7.8 EC50 = 15.8 nM Funct
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
652 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc[nH]2)cc1
CHEMBL248746 ghsr_human Human No 7.8 EC50 = 15.9 nM Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
484 5 1 7 3.8 COc1cc2c(cc1N1CCNC(C)(C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2
CHEMBL4167481 ghsr_human Human No 7.8 EC50 = 15.9 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
425 4 3 5 3.0 Cn1c(C(=O)N[C@H]2Cc3ccccc3[C@@H]2NC(=O)c2cnccc2N)cc2ccccc21
CHEMBL265950 ghsr_human Human No 7.8 EC50 = 15.9 nM Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
441 6 2 7 2.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-n2cccn2)cc1
CHEMBL402632 ghsr_human Human No 7.8 EC50 = 15.9 nM Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
458 6 2 7 3.8 COc1ccc(NS(=O)(=O)c2ccc(-c3ccccn3)s2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL481014 ghsr_human Human No 7.8 EC50 = 15.9 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
407 4 1 5 1.7 Cc1ccc(-c2ccc(S(=O)(=O)N3CC[C@H]3C(=O)N3CC[C@@H](N)C3)cc2F)o1
CHEMBL481601 ghsr_human Human No 7.8 EC50 = 15.9 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
413 4 1 4 2.5 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccccc3)cc2)C1
CHEMBL2364337 ghsr_human Human No 7.8 EC50 = 15.9 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
442 6 2 7 3.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)nc1
CHEMBL2364346 ghsr_human Human No 7.8 EC50 = 15.9 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
425 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2ccc3ccccc3c2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364348 ghsr_human Human No 7.8 EC50 = 15.9 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
401 6 2 5 3.3 COc1ccc(NS(=O)(=O)/C=C/c2ccccc2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364360 ghsr_human Human No 7.8 EC50 = 15.9 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
443 5 2 5 4.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(Cl)c1Cl
CHEMBL2364368 ghsr_human Human No 7.8 EC50 = 15.9 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
466 6 2 6 4.1 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)n3)cc2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364380 ghsr_human Human No 7.8 EC50 = 15.9 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
457 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2cccs2)c1
CHEMBL2364388 ghsr_human Human No 7.8 EC50 = 15.9 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
485 7 2 6 5.2 CC(C)Oc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1
CHEMBL2364392 ghsr_human Human No 7.8 EC50 = 15.9 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
395 4 2 4 3.8 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc4ccccc4c3)c2)C[C@@H](C)N1
CHEMBL2364447 ghsr_human Human No 7.8 EC50 = 15.9 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
447 5 2 5 4.2 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)c(F)c3)c2)C[C@@H](C)N1
CHEMBL2364476 ghsr_human Human No 7.8 EC50 = 15.9 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
477 6 2 6 4.2 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc(F)c(-c2ccco2)cc1F
CHEMBL2364488 ghsr_human Human No 7.8 EC50 = 15.9 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
427 5 3 6 3.6 C[C@H]1CN(c2ccc(O)c(NS(=O)(=O)c3ccc(-c4ccco4)cc3)c2)C[C@@H](C)N1
CHEMBL490601 ghsr_human Human No 6.8 EC50 = 150 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
372 7 1 3 3.9 CC(Oc1ccccc1)C(=O)N(Cc1ccccc1Cl)C[C@H]1CCCN1
CHEMBL402808 ghsr_human Human No 6.8 EC50 = 150 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1
CHEMBL438154 ghsr_human Human No 6.8 EC50 = 150 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
525 11 2 10 1.8 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCc2cc3ccccc3n2S(C)(=O)=O)n1
CHEMBL489610 ghsr_human Human No 5.8 EC50 = 1500 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
372 7 1 3 3.9 C[C@@H](Oc1cccc(Cl)c1)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1
CHEMBL4167267 ghsr_human Human No 5.8 EC50 = 1500 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1
CHEMBL235817 ghsr_human Human No 5.8 EC50 = 1520 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
343 8 2 8 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CC#N)n1
CHEMBL4763471 ghsr_human Human No 6.8 EC50 = 155 nM Funct
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
642 14 4 7 5.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)Cc2ccc(O)cc2)cc1
CHEMBL250973 ghsr_human Human No 6.8 EC50 = 158.5 nM Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
471 6 0 5 4.4 CCOc1ccc(CC(=O)N2CCc3cc(OC)c(N4C[C@H](C)N(C)[C@H](C)C4)cc32)cc1Cl
CHEMBL4172411 ghsr_human Human No 6.8 EC50 = 158.5 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1
CHEMBL4175534 ghsr_human Human No 6.8 EC50 = 158.5 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C
CHEMBL4637585 ghsr_human Human No 6.8 EC50 = 158.5 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
585 8 2 7 2.2 O=CN1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1
CHEMBL410282 ghsr_human Human No 6.8 EC50 = 158.5 nM Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
451 6 2 5 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2ccccc2)c1
CHEMBL1078208 ghsr_human Human No 6.8 EC50 = 158.5 nM Funct
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
440 7 2 5 3.6 CC(C)Oc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1
CHEMBL2364371 ghsr_human Human No 6.8 EC50 = 158.5 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
453 5 2 5 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(Br)c1
CHEMBL2364489 ghsr_human Human No 6.8 EC50 = 158.5 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
443 6 2 6 4.0 COc1ccc(N2CCN[C@@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1
CHEMBL403542 ghsr_human Human No 5.8 EC50 = 1580 nM Funct
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
611 11 3 7 6.6 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)Oc2ccccn2)cc1
CHEMBL4167267 ghsr_human Human No 5.8 EC50 = 1584.9 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1
CHEMBL1078207 ghsr_human Human No 5.8 EC50 = 1584.9 nM Funct
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
458 6 2 4 4.5 O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccc2)cc1
CHEMBL399651 ghsr_human Human No 7.8 EC50 = 16 nM Funct
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
571 11 2 6 6.1 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@H](NC(=O)c2ccccc2)c2c[nH]c3ccccc23)c(OC)c1
CHEMBL275795 ghsr_rat Rat No 7.8 EC50 = 16 nM Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
490 5 4 5 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CC(O)c1ccccc1O2
CHEMBL262889 ghsr_rat Rat No 7.8 EC50 = 16 nM Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
598 13 2 5 4.3 CN(C(=O)/C=C/CC(C)(C)N)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)NCC1CCCO1
CHEMBL417182 ghsr_human Human No 7.8 EC50 = 16.6 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL557206 ghsr_human Human No 7.8 EC50 = 16.6 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL417182 ghsr_human Human No 7.8 EC50 = 16.6 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL557206 ghsr_human Human No 7.8 EC50 = 16.6 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL1923612 ghsr_human Human No 7.8 EC50 = 16.6 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
508 4 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](C)N(C)C1=O
CHEMBL4517399 ghsr_human Human No 7.8 EC50 = 16.6 nM Funct
Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.36 +/- 0.01 nM)Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.36 +/- 0.01 nM)
4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O
CHEMBL1162064 ghsr_human Human No 7.8 EC50 = 17.0 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
593 13 5 5 3.6 NCCCCNC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1
CHEMBL4175534 ghsr_human Human No 6.8 EC50 = 160 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
434 9 3 5 2.3 COCCNCCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2n1C
CHEMBL2170784 ghsr_human Human No 6.8 EC50 = 161.3 nM Funct
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
None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](N)CCCCN)C(N)=O
CHEMBL3931856 ghsr_human Human No 6.8 EC50 = 163 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
508 4 4 5 2.4 CC[C@H](C)[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](C)NC1=O
CHEMBL4637585 ghsr_human Human No 6.8 EC50 = 166.4 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
585 8 2 7 2.2 O=CN1CCC[C@H](NC(=O)[C@H]2CN(S(=O)(=O)c3ccccc3)C[C@@H]2NC(=O)c2cc(-c3ccccc3Cl)on2)C1
CHEMBL2170697 ghsr_human Human No 6.8 EC50 = 168.6 nM Funct
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
None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)[C@@H](N)CCCCN)C(N)=O
CHEMBL417182 ghsr_human Human No 7.8 EC50 = 17 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL557206 ghsr_human Human No 7.8 EC50 = 17 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL237933 ghsr_human Human No 7.8 EC50 = 17 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
422 11 2 7 2.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCc1ccccc1
CHEMBL1162064 ghsr_human Human No 7.8 EC50 = 17 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
593 13 5 5 3.6 NCCCCNC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)C1CCNCC1
CHEMBL417182 ghsr_human Human No 7.8 EC50 = 17 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL557206 ghsr_human Human No 7.8 EC50 = 17 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
449 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL434609 ghsr_rat Rat No 7.8 EC50 = 17 nM Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
564 11 2 4 4.0 CNC(=O)[C@@H](Cc1ccc(F)c(F)c1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N
CHEMBL361612 ghsr_human Human No 7.8 EC50 = 17.8 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
531 10 1 4 5.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)c1ccccc1F)C(C)C
CHEMBL2170780 ghsr_human Human No 7.8 EC50 = 17.9 nM Funct
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
None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O
CHEMBL4172411 ghsr_human Human No 6.8 EC50 = 170 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
430 4 2 4 3.0 CN1CCC[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1
CHEMBL3797639 ghsr_human Human No 6.8 EC50 = 170 nM Funct
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
888 24 8 10 5.2 COc1ccc(Cn2c([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C(CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)cc1
CHEMBL380096 ghsr_human Human No 7.8 EC50 = 18 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N
CHEMBL380096 ghsr_human Human No 7.8 EC50 = 18 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N
CHEMBL611489 ghsr_human Human No 7.8 EC50 = 18 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
485 7 2 4 3.9 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C(N)=O)cc2C(F)(F)F
CHEMBL376471 ghsr_human Human No 7.8 EC50 = 18 nM Funct
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
589 12 4 6 5.6 COc1cccc(Cn2c(CCCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(C)(C)N)c1
CHEMBL1923621 ghsr_human Human No 7.8 EC50 = 18 nM Funct
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
554 3 3 5 3.1 C[C@@H]1CN[C@@H](C2CC2)C(=O)N(C)[C@H](C)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)NCCCc2ccccc2O1
CHEMBL4556887 ghsr_human Human No 7.8 EC50 = 18 nM Funct
Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.34 +/- 0.12 nM)Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.34 +/- 0.12 nM)
1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O
CHEMBL281764 ghsr_rat Rat Yes 7.8 EC50 = 18 nM Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N
CHEMBL380096 ghsr_human Human No 7.7 EC50 = 18.2 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N
CHEMBL380096 ghsr_human Human No 7.7 EC50 = 18.2 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
564 12 2 5 4.0 CN(CCc1ccccc1NS(C)(=O)=O)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N
CHEMBL611489 ghsr_human Human No 7.7 EC50 = 18.2 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
485 7 2 4 3.9 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C(N)=O)cc2C(F)(F)F
CHEMBL489819 ghsr_human Human No 6.8 EC50 = 180 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@@H](C)Oc1cccc(Cl)c1
CHEMBL391859 ghsr_human Human No 6.7 EC50 = 183 nM Funct
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
524 10 4 6 4.2 O=C(N[C@H](Cc1c[nH]c2ccccc12)C1=NNC(CCc2ccccc2)N1Cc1ccco1)C1CCNCC1
CHEMBL2170698 ghsr_human Human No 6.7 EC50 = 183.7 nM Funct
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
None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)NC(=O)[C@@H](N)CCCCN)C(N)=O
CHEMBL237302 ghsr_human Human No 5.7 EC50 = 1860 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
385 11 2 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCCCC#N)n1
CHEMBL4283858 ghsr_human Human No 6.7 EC50 = 189 nM Funct
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
475 4 2 3 5.9 Cc1ccc2c(c1)CCC2N1CCC(N(C)C(=O)N[C@@H](C)c2ccc(O)c(Cl)c2Cl)CC1
CHEMBL3578006 ghsr_human Human No 6.7 EC50 = 189.2 nM Funct
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
None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)O
CHEMBL4168863 ghsr_human Human No 7.7 EC50 = 19 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1
CHEMBL270876 ghsr_human Human No 7.7 EC50 = 19 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
464 12 2 10 1.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccn1
CHEMBL271082 ghsr_human Human No 7.7 EC50 = 19 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1
CHEMBL272085 ghsr_human Human No 7.7 EC50 = 19 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
463 12 2 9 2.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1
CHEMBL13891 ghsr_rat Rat No 7.7 EC50 = 19 nM Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
474 5 4 4 2.8 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)Cc1ccccc1C2O
CHEMBL4753592 ghsr_human Human No 7.7 EC50 = 19 nM Funct
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
656 15 4 7 5.5 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)CCc2ccc(O)cc2)cc1
CHEMBL415674 ghsr_human Human No 7.7 EC50 = 19.6 nM Funct
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
595 12 5 8 3.2 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)C3CNCCN3)=NNC2CCc2ccccc2)c(OC)c1
CHEMBL1183385 ghsr_human Human No 7.7 EC50 = 19.6 nM Funct
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
564 12 2 7 2.5 CCCCCCCC(=O)OC[C@@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12
CHEMBL294324 ghsr_human Human No 7.7 EC50 = 19.6 nM Funct
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
564 12 2 7 2.5 CCCCCCCC(=O)OC[C@@H](NC(=O)C(C)(C)N)C(=O)N1CCC2(CC1)CN(S(C)(=O)=O)c1ccccc12
CHEMBL182137 ghsr_human Human No 7.7 EC50 = 19.6 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
481 9 1 5 4.6 CCN(CC)CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C
CHEMBL434152 ghsr_human Human No 7.7 EC50 = 19.7 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
584 12 2 5 4.8 CC(=O)NC(C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C)c1ccccc1
CHEMBL251366 ghsr_human Human No 7.7 EC50 = 20.0 nM Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
478 5 1 6 3.7 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1cccc(-c3ccccn3)c1)CC2
CHEMBL4162174 ghsr_human Human No 7.7 EC50 = 20.0 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
446 4 3 4 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@H]3COCCN(C)C3)cc2c1
CHEMBL4168863 ghsr_human Human No 7.7 EC50 = 20.0 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
430 5 2 4 3.2 CN1CCC[C@H]1CC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1ccc2c(ccn2C)c1
CHEMBL4171040 ghsr_human Human No 7.7 EC50 = 20.0 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1
CHEMBL4175823 ghsr_human Human No 7.7 EC50 = 20.0 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1
CHEMBL270573 ghsr_human Human No 7.7 EC50 = 20.0 nM Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc(-c2ccco2)c1
CHEMBL1079187 ghsr_human Human No 7.7 EC50 = 20.0 nM Funct
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
452 8 2 4 4.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cnc(C)[nH]2)CC3)cc1
CHEMBL481619 ghsr_human Human No 7.7 EC50 = 20.0 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
456 5 2 5 2.0 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(NC(=O)c3ccccc3)cc2)C1
CHEMBL2364340 ghsr_human Human No 7.7 EC50 = 20.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
444 5 2 6 3.8 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccn3)cc2F)o1
CHEMBL2364373 ghsr_human Human No 7.7 EC50 = 20.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
476 6 2 7 3.9 COc1cc(F)c(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccn2)s1
CHEMBL2364393 ghsr_human Human No 7.7 EC50 = 20.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
413 4 2 4 4.0 C[C@H]1CN(c2cccc(NS(=O)(=O)c3cccc(Cl)c3Cl)c2)C[C@@H](C)N1
CHEMBL2364404 ghsr_human Human No 7.7 EC50 = 20.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
469 6 2 5 4.5 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(F)cc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364422 ghsr_human Human No 7.7 EC50 = 20.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
409 4 2 4 4.1 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cccc2ccccc12
CHEMBL2364435 ghsr_human Human No 7.7 EC50 = 20.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
469 6 2 5 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2F)cc1
CHEMBL2364440 ghsr_human Human No 7.7 EC50 = 20.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
463 5 2 5 4.7 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4cccs4)cc3F)c2)C[C@@H](C)N1
CHEMBL2364443 ghsr_human Human No 7.7 EC50 = 20.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
459 5 2 5 4.9 Cc1cc(-c2cccs2)ccc1S(=O)(=O)Nc1cc(N2C[C@H](C)N[C@H](C)C2)ccc1F
CHEMBL2364448 ghsr_human Human No 7.7 EC50 = 20.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
463 5 2 5 4.7 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)cc3Cl)c2)C[C@@H](C)N1
CHEMBL2364465 ghsr_human Human No 7.7 EC50 = 20.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
454 6 2 6 3.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccn2C)cc1
CHEMBL2364470 ghsr_human Human No 7.7 EC50 = 20.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
441 6 2 6 3.9 COc1cc(-c2ccco2)ccc1S(=O)(=O)Nc1cccc(N2C[C@H](C)N[C@H](C)C2)c1
CHEMBL2364471 ghsr_human Human No 7.7 EC50 = 20.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
457 6 2 6 4.4 COc1cc(-c2cccs2)ccc1S(=O)(=O)Nc1cccc(N2C[C@H](C)N[C@H](C)C2)c1
CHEMBL182136 ghsr_human Human No 6.7 EC50 = 190 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
480 9 1 4 4.1 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)N(C)C)C(C)C
CHEMBL4294493 ghsr_human Human No 6.7 EC50 = 194 nM Funct
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
615 6 1 6 7.1 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(-c4cnccn4)c(Cl)c3Cl)CC2)ncn1
CHEMBL4641386 ghsr_human Human No 6.7 EC50 = 199.5 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1
CHEMBL3578006 ghsr_human Human No 6.7 EC50 = 199.5 nM Funct
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
None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)O
CHEMBL1161827 ghsr_human Human No 8.7 EC50 = 2 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12
CHEMBL295984 ghsr_human Human No 8.7 EC50 = 2 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O
CHEMBL519322 ghsr_human Human No 8.7 EC50 = 2 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)[C@H](C)Oc1cccc(Cl)c1
CHEMBL4164328 ghsr_human Human No 8.7 EC50 = 2 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
390 6 3 3 2.3 CN(C)CCNC(=O)[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1
CHEMBL1161827 ghsr_human Human No 8.7 EC50 = 2 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12
CHEMBL295984 ghsr_human Human No 8.7 EC50 = 2 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
543 9 5 5 2.8 CC(C)(N)C(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(-c3ccccc3CNC(=O)NCCO)cc2)C1=O
CHEMBL4639379 ghsr_human Human No 8.7 EC50 = 2 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3C(=O)NCCN(C)C)cc2c1
CHEMBL180659 ghsr_human Human No 8.7 EC50 = 2 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
537 11 1 6 4.9 CC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C
CHEMBL180659 ghsr_human Human No 8.7 EC50 = 2 nM Funct
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
537 11 1 6 4.9 CC(=O)C(C)(C)OC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C
CHEMBL125498 ghsr_rat Rat No 8.7 EC50 = 2 nM Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
534 11 2 5 3.8 CNC(=O)[C@@H](Cc1cccs1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N
CHEMBL4640615 ghsr_human Human No 8.7 EC50 = 2.0 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL4637284 ghsr_human Human No 8.7 EC50 = 2.0 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
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
CHEMBL1161824 ghsr_human Human No 8.7 EC50 = 2.1 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12
CHEMBL1161824 ghsr_human Human No 8.7 EC50 = 2.1 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12
CHEMBL1161824 ghsr_human Human No 8.7 EC50 = 2.1 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12
CHEMBL1161824 ghsr_human Human No 8.7 EC50 = 2.1 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
508 5 3 5 2.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CC1)CS(=O)(=O)c1ccccc12
CHEMBL181832 ghsr_human Human No 8.7 EC50 = 2.1 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
557 12 1 5 5.2 COc1ccccc1CC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C
CHEMBL2170695 ghsr_human Human No 8.7 EC50 = 2.1 nM Funct
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
None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1csc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(N)=O
CHEMBL4636780 ghsr_human Human No 8.7 EC50 = 2.2 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
569 6 2 7 2.2 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N1C[C@H]2CCNC[C@H]21)c1cc(-c2ccccc2Cl)on1
CHEMBL33182 ghsr_human Human No 8.6 EC50 = 2.3 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
559 12 4 7 1.4 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)CC(=O)O)CC1
CHEMBL33182 ghsr_human Human No 8.6 EC50 = 2.3 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
559 12 4 7 1.4 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCN(c2ccccc2NS(=O)(=O)CC(=O)O)CC1
CHEMBL2113326 ghsr_human Human No 8.6 EC50 = 2.3 nM Funct
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
557 9 4 5 5.4 O=C(N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1-c1ccccc1)C1CCNCC1
CHEMBL181786 ghsr_human Human No 8.6 EC50 = 2.3 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
563 8 1 5 6.6 CC(C)N(CCNC(=O)C1c2ccc(Oc3ccc(C(F)(F)F)cc3)cc2CCN1C(=O)OC(C)(C)C)C(C)C
CHEMBL182158 ghsr_human Human No 8.6 EC50 = 2.4 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
541 9 1 6 6.3 CSc1ccc(Oc2ccc3c(c2)CCN(C(=O)OC(C)(C)C)C3C(=O)NCCN(C(C)C)C(C)C)cc1
CHEMBL241775 ghsr_human Human No 8.6 EC50 = 2.5 nM Funct
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
601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCNC2)cc1
CHEMBL4556887 ghsr_human Human No 8.6 EC50 = 2.5 nM Funct
Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.40 +/- 0.05 nM)Antagonist activity at SNAP-tagged human GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced inositol phosphate production at 1 uM by measuring ghrelin EC50 after 30 mins by HTRF assay (Rvb = 0.40 +/- 0.05 nM)
1598 47 22 19 -3.2 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)O)[C@@H](C)CC)C(C)C)[C@@H](C)O
CHEMBL1161827 ghsr_human Human No 8.6 EC50 = 2.5 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12
CHEMBL251573 ghsr_human Human No 8.6 EC50 = 2.5 nM Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
474 5 1 8 3.4 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccon3)s1)CC2
CHEMBL4164040 ghsr_human Human No 8.6 EC50 = 2.5 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1
CHEMBL1161827 ghsr_human Human No 8.6 EC50 = 2.5 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
481 7 2 4 2.9 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)C[S+]([O-])c1ccccc12
CHEMBL4636178 ghsr_human Human No 8.6 EC50 = 2.5 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
571 7 3 7 2.6 Cc1oc(-c2ccc(Cl)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1
CHEMBL4636780 ghsr_human Human No 8.6 EC50 = 2.5 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
569 6 2 7 2.2 O=C(N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N1C[C@H]2CCNC[C@H]21)c1cc(-c2ccccc2Cl)on1
CHEMBL272540 ghsr_human Human No 8.6 EC50 = 2.5 nM Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
448 6 2 8 3.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cnco2)s1
CHEMBL480639 ghsr_human Human No 8.6 EC50 = 2.5 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
463 4 1 5 3.1 Cc1ccc(-c2ccc(S(=O)(=O)N3CCCC[C@H]3C(=O)N3C[C@H](C)N[C@H](C)C3)cc2F)o1
CHEMBL2364379 ghsr_human Human No 8.6 EC50 = 2.5 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
457 6 2 6 4.4 COc1ccc(NS(=O)(=O)c2ccc(-c3ccsc3)cc2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364402 ghsr_human Human No 8.6 EC50 = 2.5 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)cc2F)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364415 ghsr_human Human No 8.6 EC50 = 2.5 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2Cl)s1
CHEMBL2364428 ghsr_human Human No 8.6 EC50 = 2.5 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
485 6 2 5 5.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccc(Cl)c2)cc1
CHEMBL2364481 ghsr_human Human No 8.6 EC50 = 2.5 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)c2)cc1F
CHEMBL1161829 ghsr_human Human No 8.6 EC50 = 2.7 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12
CHEMBL1161829 ghsr_human Human No 8.6 EC50 = 2.7 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12
CHEMBL1161829 ghsr_human Human No 8.6 EC50 = 2.7 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12
CHEMBL1161829 ghsr_human Human No 8.6 EC50 = 2.7 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
449 7 2 4 3.2 CC(C)(N)C(=O)N[C@H](CCCc1ccccc1)C(=O)N1CCC2(CC1)COc1ccccc12
CHEMBL432461 ghsr_human Human No 8.6 EC50 = 2.8 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
543 11 3 6 2.7 CC(C)S(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1
CHEMBL2170781 ghsr_human Human Yes 8.6 EC50 = 2.8 nM Funct
Inverse agonist activity at FLAG-tagged human ghrelin receptor Phe119:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Phe119:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
902 25 9 8 3.8 CC(C)C[C@@H](C(=O)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1=CNC2=CC=CC=C21)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@@H](CC4=CC=CC5=CC=CC=C54)NC(=O)[C@H](CCCCN)N
CHEMBL4636178 ghsr_human Human No 8.6 EC50 = 2.8 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
571 7 3 7 2.6 Cc1oc(-c2ccc(Cl)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1
CHEMBL432461 ghsr_human Human No 8.6 EC50 = 2.8 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
543 11 3 6 2.7 CC(C)S(=O)(=O)Nc1ccccc1N1CCN(C(=O)[C@@H](CCCc2ccccc2)NC(=O)C(C)(C)N)CC1
CHEMBL4645625 ghsr_human Human No 8.5 EC50 = 2.9 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1
CHEMBL260849 ghsr_human Human No 8.5 EC50 = 2.9 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
615 17 3 11 1.0 CN(CCc1cccc(S(=O)(=O)CCO)c1)C(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N
CHEMBL274340 ghsr_rat Rat No 8.5 EC50 = 2.9 nM Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
474 5 3 4 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(CCc3ccccc3O2)C1
CHEMBL485090 ghsr_human Human No 7.7 EC50 = 20 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
406 7 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1cccc(Cl)c1)C[C@H]1CCCN1
CHEMBL491044 ghsr_human Human No 7.7 EC50 = 20 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)[C@H](C)Oc2cccc(Cl)c2)cc1
CHEMBL491221 ghsr_human Human No 7.7 EC50 = 20 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
372 7 1 3 3.9 CC(Oc1ccccc1Cl)C(=O)N(Cc1ccccc1)C[C@H]1CCCN1
CHEMBL235793 ghsr_human Human No 7.7 EC50 = 20 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
452 10 2 9 1.5 COC(=O)C(c1ccccc1)n1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N
CHEMBL3799222 ghsr_human Human No 7.7 EC50 = 20 nM Funct
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
789 20 6 10 5.4 COC(=O)C(CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N)CCCCN)n1Cc1ccc(OC)cc1
CHEMBL1923617 ghsr_human Human No 7.7 EC50 = 20 nM Funct
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
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
CHEMBL13383 ghsr_rat Rat No 7.7 EC50 = 20 nM Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
472 5 3 4 3.0 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCCC2(Cc3ccccc3C2=O)C1
CHEMBL332414 ghsr_rat Rat No 7.7 EC50 = 20 nM Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
654 11 2 4 4.3 CNC(=O)[C@@H](Cc1ccc(I)cc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N
CHEMBL362798 ghsr_human Human No 7.7 EC50 = 20.9 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
507 10 1 4 5.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CC(C)(C)C)C(C)C
CHEMBL490009 ghsr_human Human No 6.7 EC50 = 200 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
415 7 2 4 3.9 CC(=O)Nc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2Cl)c1
CHEMBL235012 ghsr_human Human No 6.7 EC50 = 200 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
399 8 3 8 0.9 COC(=O)CCn1nnnc1[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N
CHEMBL489794 ghsr_human Human No 5.7 EC50 = 2000 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
370 7 1 4 4.0 CSc1cccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2ccccc2)c1
CHEMBL491835 ghsr_human Human No 5.7 EC50 = 2000 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
367 7 2 4 2.8 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)COc2ccccc2)cc1
CHEMBL519196 ghsr_human Human No 5.7 EC50 = 2000 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
444 9 1 4 5.3 CCC(Oc1ccccc1)C(=O)N(C[C@H]1CCCN1)c1cccc(-c2ccccc2)c1OC
CHEMBL271082 ghsr_human Human No 6.7 EC50 = 202 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
459 11 2 8 3.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(/C=C/c2ccccc2)CC#N)n1
CHEMBL409258 ghsr_human Human No 6.7 EC50 = 204 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
461 14 4 9 0.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCC(=O)O
CHEMBL4641386 ghsr_human Human No 6.7 EC50 = 204 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
476 7 3 5 1.8 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(C(=O)c4cccnc4)C[C@@H]3C(=O)NCCN(C)C)cc2c1
CHEMBL4162174 ghsr_human Human No 7.7 EC50 = 21 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
446 4 3 4 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)[C@H]3COCCN(C)C3)cc2c1
CHEMBL4171040 ghsr_human Human No 7.7 EC50 = 21 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)CCN(C)C)cc2c1
CHEMBL4175823 ghsr_human Human No 7.7 EC50 = 21 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
432 4 2 5 2.0 CN1CCO[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1
CHEMBL181337 ghsr_human Human No 7.7 EC50 = 21 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
544 10 1 6 3.4 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)S(=O)(=O)N(C)C)C(C)C
CHEMBL181352 ghsr_human Human No 7.7 EC50 = 21 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
577 10 1 6 5.0 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)S(=O)(=O)c1ccccc1)C(C)C
CHEMBL332987 ghsr_rat Rat No 7.7 EC50 = 21 nM Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
598 13 2 5 4.3 CN(C(=O)/C=C/CC(C)(C)N)[C@H](Cc1cccc2ccccc12)C(=O)N(C)[C@H](Cc1ccccc1)C(=O)NCC1CCCO1
CHEMBL4744051 ghsr_human Human No 7.7 EC50 = 21.5 nM Funct
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
677 14 3 7 6.0 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(C)cc2)cc1
CHEMBL49884 ghsr_human Human No 7.7 EC50 = 21.9 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL49884 ghsr_human Human No 7.7 EC50 = 21.9 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL376736 ghsr_human Human No 6.7 EC50 = 210 nM Funct
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
563 10 4 5 5.4 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2c[nH]c3ccccc23)n1Cc1ccc(F)cc1
CHEMBL4282719 ghsr_human Human No 5.7 EC50 = 2164 nM Funct
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
669 6 1 6 7.6 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@H](c3ccc(-c4cnccn4)c(Cl)c3Cl)C(F)(F)F)CC2)ncn1
CHEMBL178502 ghsr_human Human No 6.7 EC50 = 219 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
467 8 2 5 4.2 CC(C)NCCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C
CHEMBL49884 ghsr_human Human No 7.7 EC50 = 22 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL402086 ghsr_human Human No 7.7 EC50 = 22 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
447 11 2 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC(C#N)Cc1ccccc1
CHEMBL49884 ghsr_human Human No 7.7 EC50 = 22 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
433 6 2 3 3.3 CC(C)(N)C(=O)N[C@H](CCc1ccccc1)C(=O)N1CCC2(CCc3ccccc32)CC1
CHEMBL4517399 ghsr_human Human No 7.6 EC50 = 22.8 nM Funct
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
4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O
CHEMBL492028 ghsr_human Human No 6.7 EC50 = 220 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
372 7 1 3 3.9 CC(Oc1ccccc1)C(=O)N(Cc1ccc(Cl)cc1)C[C@H]1CCCN1
CHEMBL4163811 ghsr_human Human No 6.7 EC50 = 226 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1
CHEMBL4175360 ghsr_human Human No 7.6 EC50 = 23 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1
CHEMBL409327 ghsr_human Human No 7.6 EC50 = 23 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
493 14 3 8 1.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCc1ccccc1
CHEMBL410060 ghsr_human Human No 7.6 EC50 = 23 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
479 12 3 10 2.0 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1[C@@H](CC#N)COc1ccccc1O
CHEMBL266199 ghsr_human Human No 7.6 EC50 = 23 nM Funct
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
496 10 3 6 4.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nnc(CCc2ccccc2)n1Cc1ccco1
CHEMBL1923610 ghsr_human Human No 7.6 EC50 = 23 nM Funct
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
506 3 3 5 2.1 C[C@@H]1C(=O)N[C@H](Cc2ccccc2)C(=O)NCCCc2ccccc2OCCN[C@@H](C2CC2)C(=O)N1C
CHEMBL4761319 ghsr_human Human No 7.6 EC50 = 23 nM Funct
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
700 15 3 9 5.0 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCN3CCCCC3)n2Cc2ccc(OC)cc2)cc1
CHEMBL4162000 ghsr_human Human No 6.6 EC50 = 236 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3C(=O)NCCN(C)C)cc2c1
CHEMBL2170781 ghsr_human Human Yes 6.6 EC50 = 237.6 nM Funct
Agonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayAgonist activity at FLAG-tagged human ghrelin receptor Phe119:Ser mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
902 25 9 8 3.8 CC(C)C[C@@H](C(=O)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1=CNC2=CC=CC=C21)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@@H](CC4=CC=CC5=CC=CC=C54)NC(=O)[C@H](CCCCN)N
CHEMBL251855 ghsr_human Human No 7.6 EC50 = 24 nM Funct
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
618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1
CHEMBL403426 ghsr_human Human No 7.6 EC50 = 24 nM Funct
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
618 11 3 7 6.3 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)OC2CCOCC2)cc1
CHEMBL122420 ghsr_rat Rat No 7.6 EC50 = 24 nM Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1cccc2ccccc12)N(C)C(=O)/C=C/CC(C)(C)N
CHEMBL2170699 ghsr_human Human No 6.6 EC50 = 240.9 nM Funct
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
None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)CCCCN)C(N)=O
CHEMBL402808 ghsr_human Human No 6.6 EC50 = 244 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
461 12 2 8 2.9 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(C(CC#N)CCc2ccccc2)n1
CHEMBL404227 ghsr_human Human No 5.6 EC50 = 2470 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
447 11 2 8 2.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CC(C#N)Cc2ccccc2)n1
CHEMBL4170865 ghsr_human Human No 7.6 EC50 = 25 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1
CHEMBL13930 ghsr_rat Rat No 7.6 EC50 = 25 nM Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
474 5 3 4 3.3 CC(C)(N)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC2(CCc3ccccc3O2)CC1
CHEMBL4753046 ghsr_human Human No 7.6 EC50 = 25 nM Funct
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
732 15 4 8 6.2 COc1ccc(/C=C(\C#N)C(=O)NCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3c[nH]c4ccccc34)n2Cc2ccc(OC)cc2)cc1
CHEMBL4636229 ghsr_human Human No 7.6 EC50 = 25.1 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
585 7 1 7 3.0 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1N(C)C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1
CHEMBL4164531 ghsr_human Human No 7.6 EC50 = 25.1 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1
CHEMBL4170865 ghsr_human Human No 7.6 EC50 = 25.1 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
411 4 4 4 3.0 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2ccccc2[nH]1
CHEMBL4175360 ghsr_human Human No 7.6 EC50 = 25.1 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
448 4 4 5 2.6 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1nc2cc(F)c(F)cc2[nH]1
CHEMBL4636229 ghsr_human Human No 7.6 EC50 = 25.1 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
585 7 1 7 3.0 CN(C(=O)[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1N(C)C(=O)c1cc(-c2ccccc2Cl)on1)[C@H]1CCCNC1
CHEMBL4646979 ghsr_human Human No 7.6 EC50 = 25.1 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
523 6 4 5 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@]3(C)C(=O)N[C@H]3CCCNC3)cc2c1
CHEMBL2364344 ghsr_human Human No 7.6 EC50 = 25.1 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
476 6 2 7 4.0 COc1ccc(N2C[C@H](C)N[C@H](C)C2)nc1NS(=O)(=O)c1ccc(-c2ccoc2)cc1Cl
CHEMBL2364369 ghsr_human Human No 7.6 EC50 = 25.1 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
465 5 2 6 4.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1cc2cc(Cl)ccc2s1
CHEMBL2364383 ghsr_human Human No 7.6 EC50 = 25.1 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
444 5 3 7 3.5 C[C@H]1CN(c2ccc(O)c(NS(=O)(=O)c3ccc(-c4ccccn4)s3)c2)C[C@@H](C)N1
CHEMBL2364396 ghsr_human Human No 7.6 EC50 = 25.1 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
461 5 2 5 5.1 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-c4ccc(Cl)s4)cc3)c2)C[C@@H](C)N1
CHEMBL2364400 ghsr_human Human No 7.6 EC50 = 25.1 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
411 5 2 6 2.9 C[C@H]1CN(c2cccc(NS(=O)(=O)c3ccc(-n4cccn4)cc3)c2)C[C@@H](C)N1
CHEMBL2364410 ghsr_human Human No 7.6 EC50 = 25.1 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccccc2C)s1
CHEMBL2364412 ghsr_human Human No 7.6 EC50 = 25.1 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
485 6 2 6 5.0 COc1ccc(NS(=O)(=O)c2ccc(-c3c(C)cccc3C)s2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364421 ghsr_human Human No 7.6 EC50 = 25.1 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
477 6 2 7 4.8 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)s1
CHEMBL2364445 ghsr_human Human No 7.6 EC50 = 25.1 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
429 5 2 5 4.1 C[C@H]1CN(c2ccc(F)c(NS(=O)(=O)c3ccc(-c4ccoc4)cc3)c2)C[C@@H](C)N1
CHEMBL2364452 ghsr_human Human No 7.6 EC50 = 25.1 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
465 6 2 9 3.3 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csnn2)s1
CHEMBL4646979 ghsr_human Human No 7.6 EC50 = 25.8 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
523 6 4 5 2.2 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4ccccc4)C[C@]3(C)C(=O)N[C@H]3CCCNC3)cc2c1
CHEMBL507551 ghsr_human Human No 6.6 EC50 = 250 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
392 6 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(C[C@H]1CCCN1)c1cccc(Cl)c1
CHEMBL4160541 ghsr_human Human No 6.6 EC50 = 250 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1
CHEMBL4160541 ghsr_human Human No 6.6 EC50 = 251.2 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
416 4 2 4 2.6 CN1CC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1
CHEMBL4162000 ghsr_human Human No 6.6 EC50 = 251.2 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
404 6 3 3 2.6 Cc1ccc2[nH]c(C(=O)N[C@H]3Cc4ccccc4[C@H]3C(=O)NCCN(C)C)cc2c1
CHEMBL4163811 ghsr_human Human No 6.6 EC50 = 251.2 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
404 6 3 3 2.9 Cc1ccc2[nH]c(C(=O)N[C@@H]3Cc4ccccc4[C@H]3NC(=O)CCN(C)C)cc2c1
CHEMBL4167965 ghsr_human Human No 6.6 EC50 = 251.2 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
432 4 2 5 2.0 CN1CCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1
CHEMBL4171300 ghsr_human Human No 6.6 EC50 = 251.2 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
446 4 2 5 2.4 CN1CCCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1
CHEMBL3578014 ghsr_human Human No 6.6 EC50 = 251.2 nM Funct
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
None None None CC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O
CHEMBL241242 ghsr_human Human No 6.6 EC50 = 256 nM Funct
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
524 12 4 6 3.9 COc1ccc(CN2C([C@@H](Cc3c[nH]c4ccccc34)NC(=O)CCN)=NNC2CCc2ccccc2)cc1
CHEMBL181051 ghsr_human Human No 6.6 EC50 = 257 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
451 9 1 4 3.9 CC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C
CHEMBL369571 ghsr_human Human No 6.6 EC50 = 257 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
467 7 2 5 4.2 CC(C)(CN)CNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OC(C)(C)C
CHEMBL237059 ghsr_human Human No 6.6 EC50 = 259 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
487 11 3 9 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1Cc1ccc(NS(C)(=O)=O)cc1
CHEMBL410499 ghsr_human Human No 7.6 EC50 = 26 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
471 12 3 8 1.2 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCC(F)(F)F
CHEMBL1923638 ghsr_human Human No 7.6 EC50 = 26 nM Funct
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
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
CHEMBL366916 ghsr_human Human No 7.6 EC50 = 26.7 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
541 12 1 4 5.6 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)CCc1ccccc1)C(C)C
CHEMBL488966 ghsr_human Human No 6.6 EC50 = 260 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
406 7 1 3 4.5 CC(Oc1ccccc1Cl)C(=O)N(Cc1ccccc1Cl)C[C@H]1CCCN1
CHEMBL4171300 ghsr_human Human No 6.6 EC50 = 262 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
446 4 2 5 2.4 CN1CCCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1
CHEMBL3578014 ghsr_human Human No 6.6 EC50 = 266.8 nM Funct
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
None None None CC(=O)N[C@@H](CCCCNC(=O)CCCCCNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1cccc2ccccc12)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O
CHEMBL1923502 ghsr_human Human Yes 7.6 EC50 = 27 nM Funct
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
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
CHEMBL1963249 ghsr_human Human Yes 7.6 EC50 = 27 nM Funct
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
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
CHEMBL409894 ghsr_human Human No 7.6 EC50 = 27 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
447 14 4 9 0.1 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCCO
CHEMBL236513 ghsr_human Human No 7.6 EC50 = 27 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
479 13 3 8 1.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(=O)NCCc1ccccc1
CHEMBL270851 ghsr_human Human No 7.6 EC50 = 27 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
447 11 2 8 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC(C#N)c1ccccc1
CHEMBL1923642 ghsr_human Human No 7.6 EC50 = 27 nM Funct
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
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
CHEMBL180337 ghsr_human Human No 7.6 EC50 = 27 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
543 11 1 5 5.7 CC(C)N(CCNC(=O)C1c2ccc(OCc3ccccc3)cc2CCN1C(=O)OCc1ccccc1)C(C)C
CHEMBL4777792 ghsr_human Human No 7.6 EC50 = 27 nM Funct
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
679 14 4 8 5.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2ccc(O)cc2)cc1
CHEMBL4517399 ghsr_human Human No 7.6 EC50 = 27.7 nM Funct
Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.41 +/- 0.13 nM)Antagonist activity at human SNAP-tagged GHSR expressed in HEK293T cells assessed as reduction in ghrelin-induced calcium production at 1 uM by measuring ghrelin EC50 after 15 mins by Fluo 4-AM dye-based fluorescence assay (Rvb = 0.41 +/- 0.13 nM)
4548 115 75 66 -23.9 CCCC[C@H](N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C)C(=O)N[C@H](CO)C(=O)N[C@@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)O)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC2=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC1=O)[C@@H](C)CC)C(C)C)[C@@H](C)O
CHEMBL4167965 ghsr_human Human No 6.6 EC50 = 274 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
432 4 2 5 2.0 CN1CCO[C@@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1
CHEMBL2113317 ghsr_human Human No 6.6 EC50 = 279 nM Funct
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
524 13 3 7 4.4 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NCCN)c(OC)c1
CHEMBL4164531 ghsr_human Human No 7.6 EC50 = 28 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
430 4 2 4 3.0 CN1CCC[C@H](C(=O)N[C@H]2c3ccccc3C[C@@H]2NC(=O)c2ccc3c(ccn3C)c2)C1
CHEMBL4746362 ghsr_human Human No 7.6 EC50 = 28 nM Funct
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
702 14 4 7 6.2 COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)CNC(=O)/C(C#N)=C/c2c[nH]c3ccccc23)cc1
CHEMBL391510 ghsr_human Human No 7.5 EC50 = 29 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
343 8 2 8 0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CC#N
CHEMBL1923502 ghsr_human Human Yes 7.5 EC50 = 29 nM Funct
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
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
CHEMBL1963249 ghsr_human Human Yes 7.5 EC50 = 29 nM Funct
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
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
CHEMBL3578008 ghsr_human Human No 7.5 EC50 = 29 nM Funct
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
1002 29 10 9 3.8 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O
CHEMBL4281310 ghsr_human Human No 7.5 EC50 = 29.4 nM Funct
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
601 5 1 4 7.4 Cc1cc(-c2ccc3c(c2)CC[C@H]3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C#CC4CC4)c(Cl)c3Cl)CC2)ncn1
CHEMBL2170781 ghsr_human Human Yes 7.5 EC50 = 29.6 nM Funct
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Tyr mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
902 25 9 8 3.8 CC(C)C[C@@H](C(=O)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1=CNC2=CC=CC=C21)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@@H](CC4=CC=CC5=CC=CC=C54)NC(=O)[C@H](CCCCN)N
CHEMBL3939196 ghsr_human Human No 6.5 EC50 = 298 nM Funct
Agonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assayAgonist activity at human GSHR1a transfected in CHOK1 cells co-expressing Galpha16 assessed as increase in Ca2+ release by aequorin assay
508 5 3 5 2.5 CCC[C@@H]1NCCOc2ccccc2CCCNC(=O)[C@@H](Cc2ccccc2)NC(=O)CN(CC)C1=O
CHEMBL4280040 ghsr_human Human No 6.5 EC50 = 298 nM Funct
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
577 6 1 4 7.5 Cc1cc(-c2ccc3c(c2)CCC3N2CCC(N(C)C(=O)N[C@@H](C)c3ccc(C4CC4)c(Cl)c3Cl)CC2)ncn1
CHEMBL1162926 ghsr_human Human No 8.5 EC50 = 3 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
471 10 1 3 4.8 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)Cc1ccccc1
CHEMBL209020 ghsr_human Human Yes 8.5 EC50 = 3 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
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
CHEMBL281764 ghsr_human Human Yes 8.5 EC50 = 3 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N
CHEMBL382844 ghsr_human Human No 8.5 EC50 = 3 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1
CHEMBL1793862 ghsr_human Human No 8.5 EC50 = 3 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
None None None CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N
CHEMBL482420 ghsr_human Human No 8.5 EC50 = 3 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
386 7 1 3 4.2 Cc1ccccc1CN(C[C@H]1CCCN1)C(=O)C(C)Oc1cccc(Cl)c1
CHEMBL113313 ghsr_rat Rat Yes 8.5 EC50 = 3 nM Bind
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
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
CHEMBL4164040 ghsr_human Human No 8.5 EC50 = 3 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
447 4 4 4 3.2 Nc1ccncc1C(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2c(F)cc(F)cc2[nH]1
CHEMBL4171914 ghsr_human Human No 8.5 EC50 = 3 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
443 4 3 5 3.1 Cn1ccc2c(F)c(C(=O)N[C@H]3Cc4ccccc4[C@@H]3NC(=O)c3cnccc3N)ccc21
CHEMBL409462 ghsr_human Human No 8.5 EC50 = 3 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
539 16 4 10 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOc1cccc(C(=O)NCCCCO)c1
CHEMBL1162058 ghsr_human Human No 8.5 EC50 = 3 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
485 11 1 3 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1
CHEMBL209020 ghsr_human Human Yes 8.5 EC50 = 3 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
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
CHEMBL281764 ghsr_human Human Yes 8.5 EC50 = 3 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N
CHEMBL382844 ghsr_human Human No 8.5 EC50 = 3 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1
CHEMBL130229 ghsr_human Human No 8.5 EC50 = 3 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
None None None CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N
CHEMBL266063 ghsr_human Human No 8.5 EC50 = 3 nM Funct
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
601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1
CHEMBL266063 ghsr_human Human No 8.5 EC50 = 3 nM Funct
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
601 11 4 6 5.5 COc1ccc(Cn2c(CCc3c[nH]c4ccccc34)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C2CCNCC2)cc1
CHEMBL398570 ghsr_human Human No 8.5 EC50 = 3 nM Funct
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
435 12 4 10 -0.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCOC(=O)NCCO
CHEMBL122108 ghsr_rat Rat No 8.5 EC50 = 3 nM Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
554 12 2 4 4.2 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc(-c2ccccc2)cc1)N(C)C(=O)/C=C/CC(C)(C)N
CHEMBL1162926 ghsr_human Human No 8.5 EC50 = 3.0 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
471 10 1 3 4.8 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)Cc1ccccc1
CHEMBL209020 ghsr_human Human Yes 8.5 EC50 = 3.0 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
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
CHEMBL281764 ghsr_human Human Yes 8.5 EC50 = 3.0 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N
CHEMBL382844 ghsr_human Human No 8.5 EC50 = 3.0 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1
CHEMBL1793862 ghsr_human Human No 8.5 EC50 = 3.0 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
None None None CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N
CHEMBL1162058 ghsr_human Human No 8.5 EC50 = 3.0 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
485 11 1 3 4.9 CNC(C)(C)C/C=C/C(=O)N(C)[C@H](Cc1ccc2ccccc2c1)C(=O)N(C)CCc1ccccc1
CHEMBL209020 ghsr_human Human Yes 8.5 EC50 = 3.0 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
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
CHEMBL281764 ghsr_human Human Yes 8.5 EC50 = 3.0 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
528 11 2 4 3.7 CNC(=O)[C@@H](Cc1ccccc1)N(C)C(=O)[C@@H](Cc1ccc2ccccc2c1)N(C)C(=O)/C=C/CC(C)(C)N
CHEMBL382844 ghsr_human Human No 8.5 EC50 = 3.0 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
491 9 3 6 1.4 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)C(=O)N1CCC2=NNC(=O)[C@@]2(Cc2ccccc2)C1
CHEMBL130229 ghsr_human Human No 8.5 EC50 = 3.0 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
None None None CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)N
CHEMBL4637916 ghsr_human Human No 8.5 EC50 = 3.1 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
518 8 3 5 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCCCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1
CHEMBL263389 ghsr_human Human No 8.5 EC50 = 3.1 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
523 14 3 9 2.0 CN(CCc1cccc(O)c1)C(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N
CHEMBL254166 ghsr_human Human No 8.5 EC50 = 3.1 nM Funct
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
547 15 4 11 1.2 CC(C)(N)C(=O)N[C@H](COCc1cccc(OC(F)(F)F)c1)c1nnnn1CCOC(=O)NCCCCO
CHEMBL400124 ghsr_human Human No 8.5 EC50 = 3.2 nM Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
470 5 1 7 3.4 COc1cc2c(cc1N1CCN[C@@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2
CHEMBL4637916 ghsr_human Human No 8.5 EC50 = 3.2 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
518 8 3 5 1.3 Cc1ccc2[nH]c(C(=O)N[C@H]3CCN(S(=O)(=O)N4CCCCC4)C[C@@H]3C(=O)NCCN(C)C)cc2c1
CHEMBL4645625 ghsr_human Human No 8.5 EC50 = 3.2 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
515 8 3 7 0.6 Cc1ccc2[nH]c(C(=O)N[C@H]3CN(S(=O)(=O)c4cn(C)nc4C)C[C@@H]3C(=O)NCCN(C)C)cc2c1
CHEMBL521246 ghsr_human Human No 8.5 EC50 = 3.2 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
421 4 1 5 2.2 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccco3)c(F)c2)C1
CHEMBL2364425 ghsr_human Human No 8.5 EC50 = 3.2 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
475 6 2 6 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3cccs3)c(F)c2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364460 ghsr_human Human No 8.5 EC50 = 3.2 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
491 6 2 6 5.1 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccsc2)cc1Cl
CHEMBL2364485 ghsr_human Human No 8.5 EC50 = 3.2 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
456 6 2 7 3.6 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)o2)cn1
CHEMBL2364491 ghsr_human Human No 8.5 EC50 = 3.2 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
459 5 3 6 4.1 Cc1ccc(-c2ccc(S(=O)(=O)Nc3cc(N4C[C@H](C)N[C@H](C)C4)ccc3O)cc2F)o1
CHEMBL259016 ghsr_human Human No 8.5 EC50 = 3.3 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
501 14 4 9 -0.3 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCCC(=O)NCCN1CCNC1=O
CHEMBL237701 ghsr_human Human No 8.5 EC50 = 3.3 nM Funct
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
502 11 3 10 0.1 CC(=O)N[C@@H]1CCN(C(=O)OCCn2nnnc2[C@@H](COCc2ccccc2)NC(=O)C(C)(C)N)C1
CHEMBL2170781 ghsr_human Human Yes 8.5 EC50 = 3.3 nM Funct
Inverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Asp mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor Ser123:Asp mutant expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
902 25 9 8 3.8 CC(C)C[C@@H](C(=O)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1=CNC2=CC=CC=C21)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@@H](CC4=CC=CC5=CC=CC=C54)NC(=O)[C@H](CCCCN)N
CHEMBL180093 ghsr_human Human No 8.5 EC50 = 3.4 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
495 11 1 5 4.9 CCCOC(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C
CHEMBL360877 ghsr_human Human No 8.5 EC50 = 3.4 nM Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
541 11 1 4 5.7 CC(C(=O)N1CCc2cc(OCc3ccccc3)ccc2C1C(=O)NCCN(C(C)C)C(C)C)c1ccccc1
CHEMBL2170781 ghsr_human Human Yes 8.5 EC50 = 3.4 nM Funct
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
902 25 9 8 3.8 CC(C)C[C@@H](C(=O)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1=CNC2=CC=CC=C21)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@@H](CC4=CC=CC5=CC=CC=C54)NC(=O)[C@H](CCCCN)N
CHEMBL4791255 ghsr_human Human No 8.4 EC50 = 3.6 nM Funct
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
707 16 3 8 6.1 COc1ccc(/C=C(\C#N)C(=O)NCCC(=O)N[C@H](Cc2c[nH]c3ccccc23)c2nnc(CCc3ccccc3)n2Cc2ccc(OC)cc2)cc1
CHEMBL237492 ghsr_human Human No 8.4 EC50 = 3.8 nM Funct
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
477 14 3 10 0.6 CN(CCCCO)C(=O)OCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N
CHEMBL2170781 ghsr_human Human Yes 8.4 EC50 = 3.8 nM Funct
Inverse agonist activity at FLAG-tagged human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assayInverse agonist activity at FLAG-tagged human ghrelin receptor expressed in COS 7 cells using [2-3H]myo-inositol by inositol triphosphate turnover assay
902 25 9 8 3.8 CC(C)C[C@@H](C(=O)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1=CNC2=CC=CC=C21)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@@H](CC4=CC=CC5=CC=CC=C54)NC(=O)[C@H](CCCCN)N
CHEMBL207970 ghsr_human Human No 8.4 EC50 = 4.0 nM Bind
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O
CHEMBL248542 ghsr_human Human No 8.4 EC50 = 4.0 nM Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
470 5 1 7 3.4 COc1cc2c(cc1N1CCN[C@H](C)C1)N(S(=O)(=O)c1ccc(-c3ccccn3)s1)CC2
CHEMBL207970 ghsr_human Human No 8.4 EC50 = 4.0 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
519 10 2 6 2.1 CCN1N=C2CCN(C(=O)[C@@H](COCc3ccccc3)NC(=O)C(C)(C)N)C[C@]2(Cc2ccccc2)C1=O
CHEMBL4638566 ghsr_human Human No 8.4 EC50 = 4.0 nM Funct
Agonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assayAgonist activity at human GHSR expressed in HEK293 cells assessed as increase in IP1 accumulation measured after 90 mins in presence of LiCl by HTRF assay
605 7 3 7 3.0 Cc1oc(-c2ccc(C(F)(F)F)cc2)nc1C(=O)N[C@H]1CN(S(=O)(=O)c2ccccc2)C[C@@H]1C(=O)N[C@H]1CCCNC1
CHEMBL256263 ghsr_human Human No 8.4 EC50 = 4.0 nM Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
457 6 2 6 4.4 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1
CHEMBL401548 ghsr_human Human No 8.4 EC50 = 4.0 nM Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
441 6 2 6 3.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccco2)cc1
CHEMBL1079185 ghsr_human Human No 8.4 EC50 = 4.0 nM Funct
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
438 8 2 4 4.2 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cnc[nH]2)CC3)cc1
CHEMBL1079186 ghsr_human Human No 8.4 EC50 = 4.0 nM Funct
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
452 8 2 4 4.5 CCCCc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2[nH]cnc2C)CC3)cc1
CHEMBL519121 ghsr_human Human No 8.4 EC50 = 4.0 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
474 5 2 5 2.2 N[C@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(NC(=O)c3ccccc3F)cc2)C1
CHEMBL2364374 ghsr_human Human No 8.4 EC50 = 4.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
463 6 2 7 4.5 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)s1
CHEMBL2364413 ghsr_human Human No 8.4 EC50 = 4.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
471 6 2 6 4.7 COc1ccc(NS(=O)(=O)c2ccc(-c3cccc(C)c3)s2)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364423 ghsr_human Human No 8.4 EC50 = 4.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
441 5 2 5 4.7 Cc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2cccs2)cc1
CHEMBL2364459 ghsr_human Human No 8.4 EC50 = 4.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)cc1F
CHEMBL2364473 ghsr_human Human No 8.4 EC50 = 4.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
489 6 2 6 4.9 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2ccc(C)s2)c(F)c1
CHEMBL2364482 ghsr_human Human No 8.4 EC50 = 4.0 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
471 6 2 6 4.7 COc1ccc(N2C[C@H](C)N[C@H](C)C2)cc1NS(=O)(=O)c1ccc(-c2csc(C)c2)cc1
CHEMBL236038 ghsr_human Human No 7.5 EC50 = 30 nM Funct
Agonist activity at GHS receptorAgonist activity at GHS receptor
357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N
CHEMBL489401 ghsr_human Human No 7.5 EC50 = 30 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
415 7 2 4 3.9 CC(=O)Nc1ccc(N(C[C@H]2CCCN2)C(=O)C(C)Oc2cccc(Cl)c2)cc1
CHEMBL521176 ghsr_human Human No 7.5 EC50 = 30 nM Funct
Agonist activity at GHSRAgonist activity at GHSR
406 7 1 3 4.5 CC(Oc1cccc(Cl)c1)C(=O)N(Cc1ccc(Cl)cc1)C[C@H]1CCCN1
CHEMBL236311 ghsr_human Human No 7.5 EC50 = 30 nM Funct
Agonist activity at human GHS receptor expressed in H4 cells by FLIPR assayAgonist activity at human GHS receptor expressed in H4 cells by FLIPR assay
445 14 3 8 1.5 CCCCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N
CHEMBL236038 ghsr_human Human No 7.5 EC50 = 30 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
357 9 2 8 0.7 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnnn1CCC#N
CHEMBL236311 ghsr_human Human No 7.5 EC50 = 30 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
445 14 3 8 1.5 CCCCNC(=O)CCCn1nnnc1[C@@H](COCc1ccccc1)NC(=O)C(C)(C)N
CHEMBL608827 ghsr_human Human No 7.5 EC50 = 30 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
607 8 1 5 4.8 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N1CCOCC1)cc2C(F)(F)F
CHEMBL611488 ghsr_human Human No 7.5 EC50 = 30 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
565 8 1 4 5.0 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N(C)C)cc2C(F)(F)F
CHEMBL608827 ghsr_human Human No 7.5 EC50 = 30.2 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
607 8 1 5 4.8 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N1CCOCC1)cc2C(F)(F)F
CHEMBL611488 ghsr_human Human No 7.5 EC50 = 30.2 nM Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
565 8 1 4 5.0 CCN(CC)CCN1C(=O)[C@@](O)(c2ccc3ccccc3c2)c2c1cc(C#CCCC(=O)N(C)C)cc2C(F)(F)F
CHEMBL256236 ghsr_human Human No 6.5 EC50 = 302 nM Funct
Agonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assayAgonist activity at human GHS receptor expressed in H4 glioma cells assessed as intracellular calcium concentration by FLIPR assay
447 11 2 8 2.5 CC(C)(N)C(=O)N[C@H](COCc1ccccc1)c1nnn(CCC(C#N)c2ccccc2)n1
CHEMBL4293331 ghsr_human Human No 6.5 EC50 = 306 nM Funct
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
615 6 1 4 7.8 CC[C@H](NC(=O)N(C)C1CCN(C2CCc3cc(-c4cc(C)ncn4)ccc32)CC1)c1ccc(C#CC2CC2)c(Cl)c1Cl
CHEMBL401133 ghsr_human Human No 7.5 EC50 = 31.6 nM Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
541 5 1 5 3.4 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(S(=O)(=O)Cc1cccc(I)c1)CC2
CHEMBL4167669 ghsr_human Human No 7.5 EC50 = 31.6 nM Funct
Agonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysisAgonist activity at human GHS receptor assessed as intracellular myo-IP1 secretion after 90 mins by HTRF analysis
426 6 3 3 2.9 CN(C)CCC(=O)N[C@H]1c2ccccc2C[C@@H]1NC(=O)c1cc2cc(F)c(F)cc2[nH]1
CHEMBL481602 ghsr_human Human No 7.5 EC50 = 31.6 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
403 4 1 5 2.0 N[C@@H]1CCN(C(=O)[C@@H]2CCCCN2S(=O)(=O)c2ccc(-c3ccco3)cc2)C1
CHEMBL517081 ghsr_human Human No 7.5 EC50 = 31.6 nM Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
413 4 1 4 2.5 NC1CCN(C(=O)C2CCCCN2S(=O)(=O)c2ccc(-c3ccccc3)cc2)C1
CHEMBL3578008 ghsr_human Human No 7.5 EC50 = 31.6 nM Funct
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
1002 29 10 9 3.8 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCCCN)NC(=O)CCC(=O)O)C(N)=O
CHEMBL2364339 ghsr_human Human No 7.5 EC50 = 31.6 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
445 5 2 7 3.2 Cc1ccc(-c2ccc(S(=O)(=O)Nc3ccnc(N4C[C@H](C)N[C@H](C)C4)n3)cc2F)o1
CHEMBL2364345 ghsr_human Human No 7.5 EC50 = 31.6 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
479 5 2 6 4.9 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364347 ghsr_human Human No 7.5 EC50 = 31.6 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
425 5 2 5 3.8 COc1ccc(NS(=O)(=O)c2cccc3ccccc23)cc1N1C[C@H](C)N[C@H](C)C1
CHEMBL2364378 ghsr_human Human No 7.5 EC50 = 31.6 nM Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
463 5 2 6