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 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
436 4 1 7 2.0 CC1=CC=C(O1)C2=C(C=C(C=C2)S(=O)(=O)N3CCCCC3C(=O)N4CCC(C4)N)F
CHEMBL480821 ghsr_human Human No 10.3 EC50 = 0.1 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
436 4 1 7 2.0 CC1=CC=C(O1)C2=C(C=C(C=C2)S(=O)(=O)N3CCCCC3C(=O)N4CCC(C4)N)F
CHEMBL251572 ghsr_human Human No 9.8 EC50 = 0.2 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
485 5 1 8 3.6 CC1CN(CC(N1)C)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC=C(S4)C5=CC=CC=N5)OC
CHEMBL251572 ghsr_human Human No 9.8 EC50 = 0.2 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
485 5 1 8 3.6 CC1CN(CC(N1)C)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC=C(S4)C5=CC=CC=N5)OC
CHEMBL481013 ghsr_human Human No 9.8 EC50 = 0.2 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
436 4 1 7 2.0 CC1=CC=C(O1)C2=C(C=C(C=C2)S(=O)(=O)N3CCCCC3C(=O)N4CCC(C4)N)F
CHEMBL251572 ghsr_human Human No 9.8 EC50 = 0.2 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
485 5 1 8 3.6 CC1CN(CC(N1)C)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC=C(S4)C5=CC=CC=N5)OC
CHEMBL251572 ghsr_human Human No 9.8 EC50 = 0.2 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
485 5 1 8 3.6 CC1CN(CC(N1)C)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC=C(S4)C5=CC=CC=N5)OC
CHEMBL481013 ghsr_human Human No 9.8 EC50 = 0.2 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
436 4 1 7 2.0 CC1=CC=C(O1)C2=C(C=C(C=C2)S(=O)(=O)N3CCCCC3C(=O)N4CCC(C4)N)F
CHEMBL401134 ghsr_human Human No 9.7 EC50 = 0.2 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
479 5 1 7 3.6 CC1CN(CC(N1)C)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC=C(C=C4)C5=CC=CC=N5)OC
CHEMBL518774 ghsr_human Human No 9.7 EC50 = 0.2 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 8 1.2 CC1=CC=C(O1)C2=C(C=C(C=C2)S(=O)(=O)N3CCC(C3C(=O)N4CCC(C4)N)O)F
CHEMBL259166 ghsr_human Human No 9.7 EC50 = 0.2 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
494 16 4 9 -0.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCSCCO)N
CHEMBL410074 ghsr_human Human No 9.7 EC50 = 0.2 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
526 16 4 10 -2.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCS(=O)(=O)CCO)N
CHEMBL410085 ghsr_human Human No 9.7 EC50 = 0.2 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
510 14 4 8 0.9 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCC3=CC(=CC=C3)O)N
CHEMBL13817 ghsr_human Human Yes 9.7 EC50 = 0.2 Funct
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
529 8 2 7 1.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CN(C4=CC=CC=C34)S(=O)(=O)C)N
CHEMBL401134 ghsr_human Human No 9.7 EC50 = 0.2 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
479 5 1 7 3.6 CC1CN(CC(N1)C)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC=C(C=C4)C5=CC=CC=N5)OC
CHEMBL259166 ghsr_human Human No 9.7 EC50 = 0.2 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
494 16 4 9 -0.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCSCCO)N
CHEMBL410074 ghsr_human Human No 9.7 EC50 = 0.2 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
526 16 4 10 -2.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCS(=O)(=O)CCO)N
CHEMBL410085 ghsr_human Human No 9.7 EC50 = 0.2 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
510 14 4 8 0.9 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCC3=CC(=CC=C3)O)N
CHEMBL518774 ghsr_human Human No 9.7 EC50 = 0.2 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 8 1.2 CC1=CC=C(O1)C2=C(C=C(C=C2)S(=O)(=O)N3CCC(C3C(=O)N4CCC(C4)N)O)F
CHEMBL481796 ghsr_human Human No 9.6 EC50 = 0.3 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 1 6 1.9 CC1=CC=C(O1)C2=CC=C(C=C2)S(=O)(=O)N3CCCCC3C(=O)N4CCC(C4)N
CHEMBL481796 ghsr_human Human No 9.6 EC50 = 0.3 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 1 6 1.9 CC1=CC=C(O1)C2=CC=C(C=C2)S(=O)(=O)N3CCCCC3C(=O)N4CCC(C4)N
CHEMBL460680 ghsr_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at GHS receptorAgonist activity at GHS receptor
498 15 4 10 1.0 CC(C)(C(=O)NC(CCC(C1=CC=CC=C1)(F)F)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL460680 ghsr_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at GHS receptorAgonist activity at GHS receptor
498 15 4 10 1.0 CC(C)(C(=O)NC(CCC(C1=CC=CC=C1)(F)F)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL1162065 ghsr_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
656 12 5 5 5.4 C1CNCCC1C(=O)NC(CC2=CC3=CC=CC=C3C=C2)C(=O)NC(CC4=CC5=CC=CC=C5C=C4)C(=O)NC(C6=CC=CC=C6)C(=O)N
CHEMBL1162065 ghsr_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
656 12 5 5 5.4 C1CNCCC1C(=O)NC(CC2=CC3=CC=CC=C3C=C2)C(=O)NC(CC4=CC5=CC=CC=C5C=C4)C(=O)NC(C6=CC=CC=C6)C(=O)N
CHEMBL1162065 ghsr_human Human No 9.6 EC50 = 0.3 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
656 12 5 5 5.4 C1CNCCC1C(=O)NC(CC2=CC3=CC=CC=C3C=C2)C(=O)NC(CC4=CC5=CC=CC=C5C=C4)C(=O)NC(C6=CC=CC=C6)C(=O)N
CHEMBL270666 ghsr_human Human No 9.5 EC50 = 0.3 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
480 12 3 9 0.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2C(CC#N)COC3=CC=CC=C3O)N
CHEMBL270666 ghsr_human Human No 9.5 EC50 = 0.3 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
480 12 3 9 0.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2C(CC#N)COC3=CC=CC=C3O)N
CHEMBL482220 ghsr_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
482 4 1 5 3.6 C1CCN(C(C1)C(=O)N2CCC(C2)N)S(=O)(=O)C3=CC=C(C=C3)C4=C(C=CC(=C4)Cl)Cl
CHEMBL2364468 ghsr_human Human No 9.5 EC50 = 0.3 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
490 6 2 7 4.5 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=C(C=C(C=C3)C4=CC=C(O4)C)Cl
CHEMBL482220 ghsr_human Human No 9.5 EC50 = 0.3 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
482 4 1 5 3.6 C1CCN(C(C1)C(=O)N2CCC(C2)N)S(=O)(=O)C3=CC=C(C=C3)C4=C(C=CC(=C4)Cl)Cl
CHEMBL539929 ghsr_human Human No 9.5 EC50 = 0.3 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 16 4 9 1.1 CC(C)(C(=O)NC(COCC1=CC=CC=C1C2=CC=CC=C2)C3=NN=NN3CCOC(=O)NCCCCO)N
CHEMBL322912 ghsr_human Human No 9.5 EC50 = 0.3 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
684 14 4 5 5.8 C1CNCCC1C(=O)NC(CC2=CC3=CC=CC=C3C=C2)C(=O)NC(CC4=CC5=CC=CC=C5C=C4)C(=O)N(CCC6=CC=CC=C6)CC(=O)N
CHEMBL539929 ghsr_human Human No 9.5 EC50 = 0.3 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 16 4 9 1.1 CC(C)(C(=O)NC(COCC1=CC=CC=C1C2=CC=CC=C2)C3=NN=NN3CCOC(=O)NCCCCO)N
CHEMBL260819 ghsr_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
500 7 2 8 4.4 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=C(C=CC(=C4)OC)F
CHEMBL519301 ghsr_human Human No 9.4 EC50 = 0.4 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 7 1.6 CC1=CC=C(O1)C2=C(C=C(C=C2)S(=O)(=O)N3CCCC3C(=O)N4CCC(C4)N)F
CHEMBL2364427 ghsr_human Human No 9.4 EC50 = 0.4 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 4.8 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=C(C=C(C=C3)C4=CC(=CS4)C)C
CHEMBL13817 ghsr_human Human Yes 9.4 EC50 = 0.4 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
529 8 2 7 1.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CN(C4=CC=CC=C34)S(=O)(=O)C)N
CHEMBL260819 ghsr_human Human No 9.4 EC50 = 0.4 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
500 7 2 8 4.4 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=C(C=CC(=C4)OC)F
CHEMBL519301 ghsr_human Human No 9.4 EC50 = 0.4 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 7 1.6 CC1=CC=C(O1)C2=C(C=C(C=C2)S(=O)(=O)N3CCCC3C(=O)N4CCC(C4)N)F
CHEMBL13817 ghsr_human Human Yes 9.4 EC50 = 0.4 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
529 8 2 7 1.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CN(C4=CC=CC=C34)S(=O)(=O)C)N
CHEMBL404545 ghsr_human Human No 9.4 EC50 = 0.4 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 8 1.1 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2C(CC#N)COC3=CC=CC=C3)N
CHEMBL271876 ghsr_human Human No 9.4 EC50 = 0.4 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
465 12 2 9 0.4 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2C(CC#N)COC3=CC=CC=N3)N
CHEMBL404545 ghsr_human Human No 9.4 EC50 = 0.4 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 8 1.1 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2C(CC#N)COC3=CC=CC=C3)N
CHEMBL271876 ghsr_human Human No 9.4 EC50 = 0.4 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
465 12 2 9 0.4 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2C(CC#N)COC3=CC=CC=N3)N
CHEMBL254765 ghsr_human Human No 9.4 EC50 = 0.4 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
500 15 4 11 -0.3 CC(C)(C(=O)NC(COCC1=C(C=C(C=C1)F)F)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL254765 ghsr_human Human No 9.4 EC50 = 0.4 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
500 15 4 11 -0.3 CC(C)(C(=O)NC(COCC1=C(C=C(C=C1)F)F)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL428592 ghsr_human Human No 9.4 EC50 = 0.5 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
498 15 4 9 0.1 CC(C)(C(=O)NC(COCC1=CC=CC=C1Cl)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL428592 ghsr_human Human No 9.4 EC50 = 0.5 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
498 15 4 9 0.1 CC(C)(C(=O)NC(COCC1=CC=CC=C1Cl)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL179823 ghsr_human Human No 9.3 EC50 = 0.5 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
526 11 1 6 5.3 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)OC(C)(C)C)C=C(C=C2)OC3=CC(=CC=C3)OC)C(C)C
CHEMBL180094 ghsr_human Human No 9.3 EC50 = 0.5 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
496 10 1 5 5.4 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)OC(C)(C)C)C=C(C=C2)OC3=CC=CC=C3)C(C)C
CHEMBL180094 ghsr_human Human No 9.3 EC50 = 0.5 Funct
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
496 10 1 5 5.4 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)OC(C)(C)C)C=C(C=C2)OC3=CC=CC=C3)C(C)C
CHEMBL360547 ghsr_human Human No 9.3 EC50 = 0.5 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
526 11 1 6 5.3 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)OC(C)(C)C)C=C(C=C2)OC3=CC=C(C=C3)OC)C(C)C
CHEMBL360547 ghsr_human Human No 9.3 EC50 = 0.5 Funct
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
526 11 1 6 5.3 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)OC(C)(C)C)C=C(C=C2)OC3=CC=C(C=C3)OC)C(C)C
CHEMBL404336 ghsr_human Human No 9.3 EC50 = 0.5 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
460 11 2 7 1.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2C(CC#N)C=CC3=CC=CC=C3)N
CHEMBL404336 ghsr_human Human No 9.3 EC50 = 0.5 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
460 11 2 7 1.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2C(CC#N)C=CC3=CC=CC=C3)N
CHEMBL251169 ghsr_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
452 4 1 6 4.2 CC1CN(CC(N1)C)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC5=CC=CC=C5C=C4)OC
CHEMBL272753 ghsr_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
504 6 2 7 5.1 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=C(C=CC(=C4)Cl)F
CHEMBL480037 ghsr_human Human No 9.3 EC50 = 0.5 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 8 0.6 CC1=CC=C(O1)C2=C(C=C(C=C2)S(=O)(=O)N3CC(CC3C(=O)N4CCC(C4)N)O)F
CHEMBL2364472 ghsr_human Human No 9.3 EC50 = 0.5 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 4.1 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=C(C=C(C=C3)C4=CC=CO4)Cl
CHEMBL2364429 ghsr_human Human No 9.3 EC50 = 0.5 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
490 6 2 8 4.6 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=C(C=C(C=C3)C4=CC(=CS4)C)F
CHEMBL251169 ghsr_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
452 4 1 6 4.2 CC1CN(CC(N1)C)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC5=CC=CC=C5C=C4)OC
CHEMBL272753 ghsr_human Human No 9.3 EC50 = 0.5 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
504 6 2 7 5.1 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=C(C=CC(=C4)Cl)F
CHEMBL480037 ghsr_human Human No 9.3 EC50 = 0.5 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 8 0.6 CC1=CC=C(O1)C2=C(C=C(C=C2)S(=O)(=O)N3CC(CC3C(=O)N4CCC(C4)N)O)F
CHEMBL404354 ghsr_human Human No 9.3 EC50 = 0.5 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
478 15 4 9 -0.2 CC1=CC=CC=C1COCC(C2=NN=NN2CCOC(=O)NCCCCO)NC(=O)C(C)(C)N
CHEMBL404354 ghsr_human Human No 9.3 EC50 = 0.5 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
478 15 4 9 -0.2 CC1=CC=CC=C1COCC(C2=NN=NN2CCOC(=O)NCCCCO)NC(=O)C(C)(C)N
CHEMBL1161835 ghsr_human Human No 9.2 EC50 = 0.6 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
475 5 4 4 2.4 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CC3)CC(C5=CC=CC=C45)O)N
CHEMBL411259 ghsr_human Human No 9.2 EC50 = 0.6 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
490 17 4 8 0.1 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCCCCCO)N
CHEMBL256235 ghsr_human Human No 9.2 EC50 = 0.6 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
482 12 2 9 1.2 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2C(CC#N)COC3=CC=CC=C3F)N
CHEMBL1161835 ghsr_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
475 5 4 4 2.4 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CC3)CC(C5=CC=CC=C45)O)N
CHEMBL2113324 ghsr_human Human No 9.2 EC50 = 0.6 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
632 12 4 6 4.6 COC1=CC(=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CCNCC5)CCC6=CNC7=CC=CC=C76)OC
CHEMBL2413152 ghsr_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at GHS-R1a (unknown origin)Agonist activity at GHS-R1a (unknown origin)
475 5 4 4 2.4 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CC3)CC(C5=CC=CC=C45)O)N
CHEMBL411259 ghsr_human Human No 9.2 EC50 = 0.6 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
490 17 4 8 0.1 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCCCCCO)N
CHEMBL2113324 ghsr_human Human No 9.2 EC50 = 0.6 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
632 12 4 6 4.6 COC1=CC(=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CCNCC5)CCC6=CNC7=CC=CC=C76)OC
CHEMBL1161835 ghsr_human Human No 9.2 EC50 = 0.6 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
475 5 4 4 2.4 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CC3)CC(C5=CC=CC=C45)O)N
CHEMBL1161835 ghsr_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
475 5 4 4 2.4 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CC3)CC(C5=CC=CC=C45)O)N
CHEMBL1161835 ghsr_human Human No 9.2 EC50 = 0.6 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
475 5 4 4 2.4 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CC3)CC(C5=CC=CC=C45)O)N
CHEMBL1161835 ghsr_human Human No 9.2 EC50 = 0.6 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
475 5 4 4 2.4 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CC3)CC(C5=CC=CC=C45)O)N
CHEMBL401827 ghsr_human Human No 9.2 EC50 = 0.6 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
532 15 4 9 0.7 CC(C)(C(=O)NC(COCC1=C(C(=CC=C1)Cl)Cl)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL401827 ghsr_human Human No 9.2 EC50 = 0.6 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
532 15 4 9 0.7 CC(C)(C(=O)NC(COCC1=C(C(=CC=C1)Cl)Cl)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL2364354 ghsr_human Human No 9.2 EC50 = 0.6 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
473 6 2 8 3.8 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(S3)C4=NC(=CC=C4)C)OC
CHEMBL410135 ghsr_human Human No 9.2 EC50 = 0.6 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 13 4 8 0.6 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCNC(=O)CCC3=CC(=CC=C3)O)N
CHEMBL410135 ghsr_human Human No 9.2 EC50 = 0.6 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 13 4 8 0.6 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCNC(=O)CCC3=CC(=CC=C3)O)N
CHEMBL369329 ghsr_human Human No 9.2 EC50 = 0.7 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
541 10 1 7 5.2 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)OC(C)(C)C)C=C(C=C2)OC3=CC=CC(=C3)[N+](=O)[O-])C(C)C
CHEMBL411697 ghsr_human Human No 9.2 EC50 = 0.7 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
478 16 4 9 -1.5 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCOCCO)N
CHEMBL411697 ghsr_human Human No 9.2 EC50 = 0.7 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
478 16 4 9 -1.5 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCOCCO)N
CHEMBL254973 ghsr_human Human No 9.1 EC50 = 0.7 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
532 15 4 12 0.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1C(F)(F)F)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL254973 ghsr_human Human No 9.1 EC50 = 0.7 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
532 15 4 12 0.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1C(F)(F)F)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL178900 ghsr_human Human No 9.1 EC50 = 0.7 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
530 10 1 5 6.0 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)OC(C)(C)C)C=C(C=C2)OC3=CC=C(C=C3)Cl)C(C)C
CHEMBL379074 ghsr_human Human No 9.1 EC50 = 0.8 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
492 11 1 4 5.1 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)CCC3=CC=CS3)NC
CHEMBL2304221 ghsr_human Human No 9.1 EC50 = 0.8 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
520 10 5 5 2.8 CCNC(C1(CCCN(C1)C(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(C)(C)N)CC4=CC=CC=C4)O
CHEMBL248544 ghsr_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
499 5 1 8 3.8 CC1CN(CC(N1)(C)C)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC=C(S4)C5=CC=CC=N5)OC
CHEMBL379074 ghsr_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
492 11 1 4 5.1 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)CCC3=CC=CS3)NC
CHEMBL272993 ghsr_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
492 6 2 7 4.7 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=C(C=C(C=C3)C4=CC=CS4)Cl
CHEMBL407706 ghsr_human Human Yes 9.1 EC50 = 0.8 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
456 6 2 7 3.9 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=C(O4)C
CHEMBL407706 ghsr_human Human Yes 9.1 EC50 = 0.8 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 6 2 7 3.9 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=C(O4)C
CHEMBL2364408 ghsr_human Human No 9.1 EC50 = 0.8 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
478 6 2 8 4.5 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(S3)C4=CC(=CS4)C)OC
CHEMBL379074 ghsr_human Human No 9.1 EC50 = 0.8 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
492 11 1 4 5.1 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)CCC3=CC=CS3)NC
CHEMBL2304221 ghsr_human Human No 9.1 EC50 = 0.8 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
520 10 5 5 2.8 CCNC(C1(CCCN(C1)C(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(C)(C)N)CC4=CC=CC=C4)O
CHEMBL248544 ghsr_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
499 5 1 8 3.8 CC1CN(CC(N1)(C)C)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC=C(S4)C5=CC=CC=N5)OC
CHEMBL379074 ghsr_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
492 11 1 4 5.1 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)CCC3=CC=CS3)NC
CHEMBL310457 ghsr_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
518 9 4 4 2.8 CCNC(=O)C1(CCCN(C1)C(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(C)(C)N)CC4=CC=CC=C4
CHEMBL272993 ghsr_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
492 6 2 7 4.7 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=C(C=C(C=C3)C4=CC=CS4)Cl
CHEMBL407706 ghsr_human Human Yes 9.1 EC50 = 0.8 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
456 6 2 7 3.9 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=C(O4)C
CHEMBL407706 ghsr_human Human Yes 9.1 EC50 = 0.8 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 6 2 7 3.9 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=C(O4)C
CHEMBL379074 ghsr_human Human No 9.1 EC50 = 0.8 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
492 11 1 4 5.1 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)CCC3=CC=CS3)NC
CHEMBL2304221 ghsr_human Human No 9.1 EC50 = 0.8 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
520 10 5 5 2.8 CCNC(C1(CCCN(C1)C(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(C)(C)N)CC4=CC=CC=C4)O
CHEMBL403180 ghsr_human Human No 9.1 EC50 = 0.8 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
462 12 2 7 1.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2C(CCC3=CC=CC=C3)CC#N)N
CHEMBL379074 ghsr_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
492 11 1 4 5.1 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)CCC3=CC=CS3)NC
CHEMBL310457 ghsr_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
518 9 4 4 2.8 CCNC(=O)C1(CCCN(C1)C(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(C)(C)N)CC4=CC=CC=C4
CHEMBL3798559 ghsr_human Human No 9.1 EC50 = 0.8 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
859 20 7 8 5.3 CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CC1=CNC2=CC=CC=C21)C3=NN=C(N3CC4=CC=C(C=C4)OC)C(CC5=CNC6=CC=CC=C65)NC(=O)C(C)(C)N)NC(=O)C
CHEMBL403180 ghsr_human Human No 9.1 EC50 = 0.8 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
462 12 2 7 1.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2C(CCC3=CC=CC=C3)CC#N)N
CHEMBL310457 ghsr_human Human No 9.1 EC50 = 0.8 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
518 9 4 4 2.8 CCNC(=O)C1(CCCN(C1)C(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(C)(C)N)CC4=CC=CC=C4
CHEMBL3798559 ghsr_human Human No 9.1 EC50 = 0.8 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
859 20 7 8 5.3 CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CC1=CNC2=CC=CC=C21)C3=NN=C(N3CC4=CC=C(C=C4)OC)C(CC5=CNC6=CC=CC=C65)NC(=O)C(C)(C)N)NC(=O)C
CHEMBL179785 ghsr_human Human No 9.1 EC50 = 0.9 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
567 12 1 6 4.4 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)OC(C)(C)C(=O)N(C)C)C=C(C=C2)OCC3=CC=CC=C3)C(C)C
CHEMBL471751 ghsr_human Human No 9.1 EC50 = 0.9 Funct
Agonist activity at GHS receptorAgonist activity at GHS receptor
391 9 2 8 0.9 CC(C)(C(=O)NC(CCC(C1=CC=CC=C1)(F)F)C2=NN=NN2CCC#N)N
CHEMBL113313 ghsr_human Human Yes 9.1 EC50 = 0.9 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
506 9 2 6 1.1 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3=NN(C(=O)C3(C2)CC4=CC=CC=C4)C)N
CHEMBL262358 ghsr_human Human No 9.1 EC50 = 0.9 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
540 16 4 9 0.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCOC3=CC=CC=C3C(=O)NCCCCO)N
CHEMBL471751 ghsr_human Human No 9.1 EC50 = 0.9 Funct
Agonist activity at GHS receptorAgonist activity at GHS receptor
391 9 2 8 0.9 CC(C)(C(=O)NC(CCC(C1=CC=CC=C1)(F)F)C2=NN=NN2CCC#N)N
CHEMBL262358 ghsr_human Human No 9.1 EC50 = 0.9 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
540 16 4 9 0.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCOC3=CC=CC=C3C(=O)NCCCCO)N
CHEMBL113313 ghsr_human Human Yes 9.0 EC50 = 0.9 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
506 9 2 6 1.1 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3=NN(C(=O)C3(C2)CC4=CC=CC=C4)C)N
CHEMBL47938 ghsr_human Human No 9.0 EC50 = 1 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
514 7 4 4 2.8 CC(C)(C(=O)NC1CCC2=CC=CC=C2N(C1=O)CC3=CC=C(C=C3)C4=CC=CC=C4CNC(=O)NC)N
CHEMBL1162063 ghsr_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
535 11 4 6 2.1 C1CSC2=CC=CC=C2N(C1=O)CCCC(=O)NC(CC3=CC=CC4=CC=CC=C43)C(=O)NCC(CN)O
CHEMBL47938 ghsr_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
514 7 4 4 2.8 CC(C)(C(=O)NC1CCC2=CC=CC=C2N(C1=O)CC3=CC=C(C=C3)C4=CC=CC=C4CNC(=O)NC)N
CHEMBL1923609 ghsr_human Human No 9.0 EC50 = 1 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 5 4.2 CCC(C)C1C(=O)N(C(C(=O)NC(C(=O)NCCCC2=CC=CC=C2OCCN1)CC3=CC=CC=C3)C)C
CHEMBL1923617 ghsr_human Human No 9.0 EC50 = 1 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
557 4 3 5 4.8 CCC(C)C1C(=O)N(C(C(=O)NC(C(=O)NCCCC2=CC=CC=C2OCCN1)CC3=CC=C(C=C3)Cl)C)C
CHEMBL1963249 ghsr_human Human Yes 9.0 EC50 = 1 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
539 3 3 6 3.8 CC1CNC(C(=O)N(C(C(=O)NC(C(=O)NCCCC2=CC=CC=C2O1)CC3=CC=C(C=C3)F)C)C)C4CC4
CHEMBL517543 ghsr_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
450 4 1 7 2.6 C1CCN(C(C1)C(=O)N2CCC(C2)N)S(=O)(=O)C3=CC=C(C=C3)C4=C(C=CC(=C4)F)F
CHEMBL237699 ghsr_human Human No 9.0 EC50 = 1 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
462 11 3 9 -0.9 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCOC(=O)N3CCC(C3)O)N
CHEMBL47938 ghsr_human Human No 9.0 EC50 = 1 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
514 7 4 4 2.8 CC(C)(C(=O)NC1CCC2=CC=CC=C2N(C1=O)CC3=CC=C(C=C3)C4=CC=CC=C4CNC(=O)NC)N
CHEMBL1162063 ghsr_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
535 11 4 6 2.1 C1CSC2=CC=CC=C2N(C1=O)CCCC(=O)NC(CC3=CC=CC4=CC=CC=C43)C(=O)NCC(CN)O
CHEMBL47938 ghsr_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
514 7 4 4 2.8 CC(C)(C(=O)NC1CCC2=CC=CC=C2N(C1=O)CC3=CC=C(C=C3)C4=CC=CC=C4CNC(=O)NC)N
CHEMBL517543 ghsr_human Human No 9.0 EC50 = 1 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
450 4 1 7 2.6 C1CCN(C(C1)C(=O)N2CCC(C2)N)S(=O)(=O)C3=CC=C(C=C3)C4=C(C=CC(=C4)F)F
CHEMBL237699 ghsr_human Human No 9.0 EC50 = 1 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
462 11 3 9 -0.9 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCOC(=O)N3CCC(C3)O)N
CHEMBL2364353 ghsr_human Human No 9.0 EC50 = 1 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 4.1 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=CS4)OC
CHEMBL2364403 ghsr_human Human No 9.0 EC50 = 1 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 4.5 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=C(C=C(C=C3)C4=CC=CS4)C)OC
CHEMBL2364382 ghsr_human Human No 9.0 EC50 = 1 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 4.4 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(S3)C4=CC=CC=C4)OC
CHEMBL2364338 ghsr_human Human No 9.0 EC50 = 1 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 8 3.6 CC1CN(CC(N1)C)C2=NC(=CC=C2)NS(=O)(=O)C3=CC(=C(C=C3)C4=CC=C(O4)C)F
CHEMBL414394 ghsr_human Human No 9.0 EC50 = 1.0 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
559 16 4 11 0.3 CC1=C(C(=NO1)C)C2=CC=CC=C2COCC(C3=NN=NN3CCOC(=O)NCCCCO)NC(=O)C(C)(C)N
CHEMBL414394 ghsr_human Human No 9.0 EC50 = 1.0 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
559 16 4 11 0.3 CC1=C(C(=NO1)C)C2=CC=CC=C2COCC(C3=NN=NN3CCOC(=O)NCCCCO)NC(=O)C(C)(C)N
CHEMBL1161828 ghsr_human Human No 9.0 EC50 = 1.1 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
498 7 2 5 2.7 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CS(=O)(=O)C4=CC=CC=C34)N
CHEMBL1161828 ghsr_human Human No 9.0 EC50 = 1.1 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
498 7 2 5 2.7 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CS(=O)(=O)C4=CC=CC=C34)N
CHEMBL1161828 ghsr_human Human No 9.0 EC50 = 1.1 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
498 7 2 5 2.7 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CS(=O)(=O)C4=CC=CC=C34)N
CHEMBL1161828 ghsr_human Human No 9.0 EC50 = 1.1 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
498 7 2 5 2.7 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CS(=O)(=O)C4=CC=CC=C34)N
CHEMBL1161828 ghsr_human Human No 9.0 EC50 = 1.1 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
498 7 2 5 2.7 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CS(=O)(=O)C4=CC=CC=C34)N
CHEMBL1161828 ghsr_human Human No 9.0 EC50 = 1.1 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
498 7 2 5 2.7 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CS(=O)(=O)C4=CC=CC=C34)N
CHEMBL254565 ghsr_human Human No 9.0 EC50 = 1.1 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
494 16 4 10 -0.6 CC(C)(C(=O)NC(COCC1=CC=CC=C1OC)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL254565 ghsr_human Human No 9.0 EC50 = 1.1 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
494 16 4 10 -0.6 CC(C)(C(=O)NC(COCC1=CC=CC=C1OC)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL13675 ghsr_rat Rat No 8.9 EC50 = 1.2 Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
491 5 4 5 2.2 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCCC4(C3)CC(C5=CC=CC=C5O4)O)N
CHEMBL275093 ghsr_rat Rat No 8.9 EC50 = 1.2 Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
489 5 3 5 2.4 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCCC4(C3)CC(=O)C5=CC=CC=C5O4)N
CHEMBL516602 ghsr_human Human No 8.9 EC50 = 1.3 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
419 4 2 7 0.4 CC1=CC=C(O1)C2=CC=C(C=C2)S(=O)(=O)N3CCNCC3C(=O)N4CCC(C4)N
CHEMBL516602 ghsr_human Human No 8.9 EC50 = 1.3 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
419 4 2 7 0.4 CC1=CC=C(O1)C2=CC=C(C=C2)S(=O)(=O)N3CCNCC3C(=O)N4CCC(C4)N
CHEMBL2364432 ghsr_human Human No 8.9 EC50 = 1.3 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 4.5 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(C=C3)C4=CC(=CS4)C)OC
CHEMBL2364424 ghsr_human Human No 8.9 EC50 = 1.3 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 5 2 6 4.8 CC1CN(CC(N1)C)C2=CC(=C(C=C2)C)NS(=O)(=O)C3=CC=C(C=C3)C4=CC(=CS4)C
CHEMBL254363 ghsr_human Human No 8.9 EC50 = 1.3 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
489 15 4 10 -0.8 CC(C)(C(=O)NC(COCC1=CC=CC=C1C#N)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL254363 ghsr_human Human No 8.9 EC50 = 1.3 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
489 15 4 10 -0.8 CC(C)(C(=O)NC(COCC1=CC=CC=C1C#N)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL209360 ghsr_human Human No 8.9 EC50 = 1.3 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
466 7 3 5 1.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CC(C4=CC=CC=C34)O)N
CHEMBL261358 ghsr_human Human No 8.9 EC50 = 1.3 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
476 16 4 8 -0.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCCCCO)N
CHEMBL13817 ghsr_human Human Yes 8.9 EC50 = 1.3 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
529 8 2 7 1.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CN(C4=CC=CC=C34)S(=O)(=O)C)N
CHEMBL3218890 ghsr_human Human No 8.9 EC50 = 1.3 Funct
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
473 6 0 6 3.7 CC1=C(C=CC=N1)C2=NC3=CN(N=C3C(=O)N2CC4CCCN(C4)C(C)C)C5=CC(=CC=C5)OC
CHEMBL261358 ghsr_human Human No 8.9 EC50 = 1.3 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
476 16 4 8 -0.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCCCCO)N
CHEMBL13817 ghsr_human Human Yes 8.9 EC50 = 1.3 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
529 8 2 7 1.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CN(C4=CC=CC=C34)S(=O)(=O)C)N
CHEMBL13817 ghsr_rat Rat Yes 8.9 EC50 = 1.3 Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
529 8 2 7 1.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CN(C4=CC=CC=C34)S(=O)(=O)C)N
CHEMBL209360 ghsr_human Human No 8.9 EC50 = 1.3 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
466 7 3 5 1.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CC(C4=CC=CC=C34)O)N
CHEMBL209360 ghsr_human Human No 8.9 EC50 = 1.3 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
466 7 3 5 1.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CC(C4=CC=CC=C34)O)N
CHEMBL13817 ghsr_human Human Yes 8.9 EC50 = 1.3 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
529 8 2 7 1.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CN(C4=CC=CC=C34)S(=O)(=O)C)N
CHEMBL258761 ghsr_human Human No 8.9 EC50 = 1.4 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
497 14 4 10 -2.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCS(=O)(=O)N)N
CHEMBL500468 ghsr_human Human Yes 8.9 EC50 = 1.4 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
3315 119 46 51 -18.7 CCCCCCCC(=O)OCC(C(=O)NC(CO)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)N2CCCC2C(=O)NC(CCC(=O)O)C(=O)NC(CC3=CN=CN3)C(=O)NC(CCC(=O)N)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CCC(=O)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)O)C(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)N4CCCC4C(=O)N5CCCC5C(=O)NC(C)C(=O)NC(CCCCN)C(=O)NC(CC(C)C)C(=O)NC(CCC(=O)N)C(=O)N6CCCC6C(=O)O)NC(=O)CNC(=O)C(CCCNC(=N)N)N
CHEMBL258761 ghsr_human Human No 8.9 EC50 = 1.4 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
497 14 4 10 -2.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCS(=O)(=O)N)N
CHEMBL500468 ghsr_human Human Yes 8.9 EC50 = 1.4 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
3315 119 46 51 -18.7 CCCCCCCC(=O)OCC(C(=O)NC(CO)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)N2CCCC2C(=O)NC(CCC(=O)O)C(=O)NC(CC3=CN=CN3)C(=O)NC(CCC(=O)N)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CCC(=O)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)O)C(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)N4CCCC4C(=O)N5CCCC5C(=O)NC(C)C(=O)NC(CCCCN)C(=O)NC(CC(C)C)C(=O)NC(CCC(=O)N)C(=O)N6CCCC6C(=O)O)NC(=O)CNC(=O)C(CCCNC(=N)N)N
CHEMBL500468 ghsr_human Human Yes 8.9 EC50 = 1.4 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
3315 119 46 51 -18.7 CCCCCCCC(=O)OCC(C(=O)NC(CO)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)N2CCCC2C(=O)NC(CCC(=O)O)C(=O)NC(CC3=CN=CN3)C(=O)NC(CCC(=O)N)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CCC(=O)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)O)C(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)N4CCCC4C(=O)N5CCCC5C(=O)NC(C)C(=O)NC(CCCCN)C(=O)NC(CC(C)C)C(=O)NC(CCC(=O)N)C(=O)N6CCCC6C(=O)O)NC(=O)CNC(=O)C(CCCNC(=N)N)N
CHEMBL180246 ghsr_human Human No 8.9 EC50 = 1.4 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
524 11 1 6 4.8 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)OC(C)(C)C)C=C(C=C2)OC3=CC=C(C=C3)C=O)C(C)C
CHEMBL500468 ghsr_human Human Yes 8.9 EC50 = 1.4 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
3315 119 46 51 -18.7 CCCCCCCC(=O)OCC(C(=O)NC(CO)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)N2CCCC2C(=O)NC(CCC(=O)O)C(=O)NC(CC3=CN=CN3)C(=O)NC(CCC(=O)N)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CCC(=O)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)O)C(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)N4CCCC4C(=O)N5CCCC5C(=O)NC(C)C(=O)NC(CCCCN)C(=O)NC(CC(C)C)C(=O)NC(CCC(=O)N)C(=O)N6CCCC6C(=O)O)NC(=O)CNC(=O)C(CCCNC(=N)N)N
CHEMBL500468 ghsr_human Human Yes 8.9 EC50 = 1.4 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
3315 119 46 51 -18.7 CCCCCCCC(=O)OCC(C(=O)NC(CO)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)N2CCCC2C(=O)NC(CCC(=O)O)C(=O)NC(CC3=CN=CN3)C(=O)NC(CCC(=O)N)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CCC(=O)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)O)C(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)N4CCCC4C(=O)N5CCCC5C(=O)NC(C)C(=O)NC(CCCCN)C(=O)NC(CC(C)C)C(=O)NC(CCC(=O)N)C(=O)N6CCCC6C(=O)O)NC(=O)CNC(=O)C(CCCNC(=N)N)N
CHEMBL500468 ghsr_human Human Yes 8.9 EC50 = 1.4 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
3315 119 46 51 -18.7 CCCCCCCC(=O)OCC(C(=O)NC(CO)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)N2CCCC2C(=O)NC(CCC(=O)O)C(=O)NC(CC3=CN=CN3)C(=O)NC(CCC(=O)N)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CCC(=O)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)O)C(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)N4CCCC4C(=O)N5CCCC5C(=O)NC(C)C(=O)NC(CCCCN)C(=O)NC(CC(C)C)C(=O)NC(CCC(=O)N)C(=O)N6CCCC6C(=O)O)NC(=O)CNC(=O)C(CCCNC(=N)N)N
CHEMBL500468 ghsr_human Human Yes 8.9 EC50 = 1.4 Funct
Agonist activity at GHS receptorAgonist activity at GHS receptor
3315 119 46 51 -18.7 CCCCCCCC(=O)OCC(C(=O)NC(CO)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)N2CCCC2C(=O)NC(CCC(=O)O)C(=O)NC(CC3=CN=CN3)C(=O)NC(CCC(=O)N)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CCC(=O)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)O)C(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)N4CCCC4C(=O)N5CCCC5C(=O)NC(C)C(=O)NC(CCCCN)C(=O)NC(CC(C)C)C(=O)NC(CCC(=O)N)C(=O)N6CCCC6C(=O)O)NC(=O)CNC(=O)C(CCCNC(=N)N)N
CHEMBL500468 ghsr_human Human Yes 8.9 EC50 = 1.4 Funct
Agonist activity at GHS receptorAgonist activity at GHS receptor
3315 119 46 51 -18.7 CCCCCCCC(=O)OCC(C(=O)NC(CO)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)N2CCCC2C(=O)NC(CCC(=O)O)C(=O)NC(CC3=CN=CN3)C(=O)NC(CCC(=O)N)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CCC(=O)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)O)C(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)N4CCCC4C(=O)N5CCCC5C(=O)NC(C)C(=O)NC(CCCCN)C(=O)NC(CC(C)C)C(=O)NC(CCC(=O)N)C(=O)N6CCCC6C(=O)O)NC(=O)CNC(=O)C(CCCNC(=N)N)N
CHEMBL13817 ghsr_human Human Yes 8.9 EC50 = 1.4 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
529 8 2 7 1.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CN(C4=CC=CC=C34)S(=O)(=O)C)N
CHEMBL181764 ghsr_human Human No 8.8 EC50 = 1.5 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
554 13 1 7 4.8 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)OC(C)(C)C(=O)OC)C=C(C=C2)OCC3=CC=CC=C3)C(C)C
CHEMBL181063 ghsr_human Human No 8.8 EC50 = 1.5 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
564 10 1 8 6.2 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)OC(C)(C)C)C=C(C=C2)OC3=CC=CC(=C3)C(F)(F)F)C(C)C
CHEMBL181764 ghsr_human Human No 8.8 EC50 = 1.5 Funct
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
554 13 1 7 4.8 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)OC(C)(C)C(=O)OC)C=C(C=C2)OCC3=CC=CC=C3)C(C)C
CHEMBL122939 ghsr_rat Rat No 8.8 EC50 = 1.5 Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
607 14 3 6 3.7 CC(CNC(=O)C(CC1=CC=CS1)N(C)C(=O)C(CC2=CCC(C=C2)C3=CC=CC=C3)N(C)C(=O)C=CCC(C)(C)N)O
CHEMBL433087 ghsr_human Human No 8.8 EC50 = 1.6 Funct
Activity at human 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 3 5 3.4 CCOC(=O)C1(CCCN(C1)C(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(C)(C)N)CC4=CC=CC=C4
CHEMBL433087 ghsr_human Human No 8.8 EC50 = 1.6 Funct
Activity at human 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 3 5 3.4 CCOC(=O)C1(CCCN(C1)C(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(C)(C)N)CC4=CC=CC=C4
CHEMBL79263 ghsr_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
519 10 3 5 3.4 CCOC(=O)C1(CCCN(C1)C(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(C)(C)N)CC4=CC=CC=C4
CHEMBL2364475 ghsr_human Human No 8.8 EC50 = 1.6 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
446 5 2 6 4.1 CC1CN(CC(N1)C)C2=CC(=C(C=C2)Cl)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=CO4
CHEMBL2364381 ghsr_human Human No 8.8 EC50 = 1.6 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
464 6 2 8 4.1 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(S3)C4=CSC=C4)OC
CHEMBL2364384 ghsr_human Human No 8.8 EC50 = 1.6 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 2 6 4.6 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC4=C(C=C3)C(=CC=C4)Cl
CHEMBL2364426 ghsr_human Human No 8.8 EC50 = 1.6 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
478 6 2 8 4.5 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(S3)C4=CC=C(S4)C)OC
CHEMBL2364430 ghsr_human Human No 8.8 EC50 = 1.6 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 6 2 8 3.6 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=C(C=C(C=C3)C4=CC=CO4)F
CHEMBL433087 ghsr_human Human No 8.8 EC50 = 1.6 Funct
Activity at human 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 3 5 3.4 CCOC(=O)C1(CCCN(C1)C(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(C)(C)N)CC4=CC=CC=C4
CHEMBL266063 ghsr_human Human No 8.8 EC50 = 1.6 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
602 11 4 5 4.7 COC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CCNCC5)CCC6=CNC7=CC=CC=C76
CHEMBL79263 ghsr_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
519 10 3 5 3.4 CCOC(=O)C1(CCCN(C1)C(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(C)(C)N)CC4=CC=CC=C4
CHEMBL240509 ghsr_human Human No 8.8 EC50 = 1.6 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 4 5 5.3 COC1=CC=C(C=C1)CN2C(NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CCNCC5)CCC6=CC=CC=C6
CHEMBL254766 ghsr_human Human No 8.8 EC50 = 1.6 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
498 15 4 9 0.1 CC(C)(C(=O)NC(COCC1=CC(=CC=C1)Cl)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL266063 ghsr_human Human No 8.8 EC50 = 1.6 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
602 11 4 5 4.7 COC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CCNCC5)CCC6=CNC7=CC=CC=C76
CHEMBL79263 ghsr_human Human No 8.8 EC50 = 1.6 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
519 10 3 5 3.4 CCOC(=O)C1(CCCN(C1)C(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(C)(C)N)CC4=CC=CC=C4
CHEMBL240509 ghsr_human Human No 8.8 EC50 = 1.6 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 4 5 5.3 COC1=CC=C(C=C1)CN2C(NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CCNCC5)CCC6=CC=CC=C6
CHEMBL254766 ghsr_human Human No 8.8 EC50 = 1.6 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
498 15 4 9 0.1 CC(C)(C(=O)NC(COCC1=CC(=CC=C1)Cl)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL254566 ghsr_human Human No 8.8 EC50 = 1.7 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
470 15 4 9 0.3 CC(C)(C(=O)NC(COCC1CCCCC1)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL254566 ghsr_human Human No 8.8 EC50 = 1.7 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
470 15 4 9 0.3 CC(C)(C(=O)NC(COCC1CCCCC1)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL105462 ghsr_rat Rat Yes 8.8 EC50 = 1.7 Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
873 23 11 9 1.9 CC(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCCN)C(=O)N)NC(=O)C(CC4=CNC5=CC=CC=C54)NC(=O)C(CC6=CN=CN6)N
CHEMBL253965 ghsr_human Human No 8.8 EC50 = 1.8 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
532 15 4 12 0.3 CC(C)(C(=O)NC(COCC1=CC(=CC=C1)C(F)(F)F)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL253965 ghsr_human Human No 8.8 EC50 = 1.8 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
532 15 4 12 0.3 CC(C)(C(=O)NC(COCC1=CC(=CC=C1)C(F)(F)F)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL261544 ghsr_human Human No 8.7 EC50 = 1.8 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
462 15 4 8 -0.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCCCO)N
CHEMBL133848 ghsr_human Human No 8.7 EC50 = 1.8 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
510 9 4 4 4.7 C1CNCCC1C(=O)NC(CC2=CC3=CC=CC=C3C=C2)C(=O)NC(CC4=CC5=CC=CC=C5C=C4)CO
CHEMBL261544 ghsr_human Human No 8.8 EC50 = 1.8 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
462 15 4 8 -0.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCCCO)N
CHEMBL133848 ghsr_human Human No 8.8 EC50 = 1.8 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
510 9 4 4 4.7 C1CNCCC1C(=O)NC(CC2=CC3=CC=CC=C3C=C2)C(=O)NC(CC4=CC5=CC=CC=C5C=C4)CO
CHEMBL13687 ghsr_rat Rat No 8.8 EC50 = 1.8 Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
489 5 3 5 2.4 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCCC4(C3)CC(=O)C5=CC=CC=C5O4)N
CHEMBL331093 ghsr_rat Rat No 8.8 EC50 = 1.8 Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
569 13 2 4 5.0 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)C(CC3=CC=CC=C3)C(=O)NCC4CC4)N
CHEMBL133848 ghsr_human Human No 8.7 EC50 = 1.8 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
510 9 4 4 4.7 C1CNCCC1C(=O)NC(CC2=CC3=CC=CC=C3C=C2)C(=O)NC(CC4=CC5=CC=CC=C5C=C4)CO
CHEMBL398372 ghsr_human Human No 8.7 EC50 = 1.9 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
464 15 4 9 -0.5 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL398372 ghsr_human Human No 8.7 EC50 = 1.9 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
464 15 4 9 -0.5 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL398372 ghsr_human Human No 8.7 EC50 = 1.9 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
464 15 4 9 -0.5 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL398372 ghsr_human Human No 8.7 EC50 = 1.9 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
464 15 4 9 -0.5 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL398372 ghsr_human Human No 8.7 EC50 = 1.9 Funct
Agonist activity at GHS receptorAgonist activity at GHS receptor
464 15 4 9 -0.5 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL398372 ghsr_human Human No 8.7 EC50 = 1.9 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
464 15 4 9 -0.5 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL398372 ghsr_human Human No 8.7 EC50 = 1.9 Funct
Agonist activity at GHS receptorAgonist activity at GHS receptor
464 15 4 9 -0.5 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL398372 ghsr_human Human No 8.7 EC50 = 1.9 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
464 15 4 9 -0.5 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL295984 ghsr_human Human No 8.7 EC50 = 2.0 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
544 9 5 5 2.1 CC(C)(C(=O)NC1CCC2=CC=CC=C2N(C1=O)CC3=CC=C(C=C3)C4=CC=CC=C4CNC(=O)NCCO)N
CHEMBL295984 ghsr_human Human No 8.7 EC50 = 2.0 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
544 9 5 5 2.1 CC(C)(C(=O)NC1CCC2=CC=CC=C2N(C1=O)CC3=CC=C(C=C3)C4=CC=CC=C4CNC(=O)NCCO)N
CHEMBL1162063 ghsr_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
535 11 4 6 2.1 C1CSC2=CC=CC=C2N(C1=O)CCCC(=O)NC(CC3=CC=CC4=CC=CC=C43)C(=O)NCC(CN)O
CHEMBL295984 ghsr_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
544 9 5 5 2.1 CC(C)(C(=O)NC1CCC2=CC=CC=C2N(C1=O)CC3=CC=C(C=C3)C4=CC=CC=C4CNC(=O)NCCO)N
CHEMBL261030 ghsr_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
482 7 2 7 4.3 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CC(=CC=C4)OC
CHEMBL270790 ghsr_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
476 6 2 8 4.2 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=C(C=C(C=C3)C4=CC=CS4)F
CHEMBL261030 ghsr_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
482 7 2 7 4.3 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CC(=CC=C4)OC
CHEMBL270790 ghsr_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
476 6 2 8 4.2 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=C(C=C(C=C3)C4=CC=CS4)F
CHEMBL481620 ghsr_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
487 6 2 7 1.5 COC1=CC=CC(=C1)C(=O)NC2=CC=C(C=C2)S(=O)(=O)N3CCCCC3C(=O)N4CCC(C4)N
CHEMBL481620 ghsr_human Human No 8.7 EC50 = 2.0 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
487 6 2 7 1.5 COC1=CC=CC(=C1)C(=O)NC2=CC=C(C=C2)S(=O)(=O)N3CCCCC3C(=O)N4CCC(C4)N
CHEMBL2364407 ghsr_human Human No 8.7 EC50 = 2.0 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
478 6 2 8 4.5 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(S3)C4=CC(=CS4)C
CHEMBL2364480 ghsr_human Human No 8.7 EC50 = 2.0 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
490 6 2 8 4.6 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC(=C(C=C3)C4=CSC(=C4)C)F
CHEMBL2364441 ghsr_human Human No 8.7 EC50 = 2.0 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 3.8 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=C(C=C(C=C3)C4=CC=CO4)C
CHEMBL2364399 ghsr_human Human No 8.7 EC50 = 2.0 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
464 6 2 8 4.1 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(S3)C4=CC=CS4)OC
CHEMBL1161825 ghsr_human Human No 8.0 EC50 = 10 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
468 7 2 5 2.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CSC4=CC=CC=C34)N
CHEMBL294923 ghsr_human Human No 8.0 EC50 = 10 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
448 7 2 3 4.3 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CCC4=CC=CC=C43)CC2)N
CHEMBL488965 ghsr_human Human No 8.0 EC50 = 10 Funct
Agonist activity at GHSRAgonist activity at GHSR
407 7 1 3 4.7 CC(C(=O)N(CC1CCCN1)CC2=CC(=CC=C2)Cl)OC3=CC=CC=C3Cl
CHEMBL248745 ghsr_human Human No 8.0 EC50 = 10 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
499 5 1 8 3.8 CC1CN(CC(N1)(C)C)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC=C(S4)C5=CC=CC=N5)OC
CHEMBL237926 ghsr_human Human No 8.0 EC50 = 10 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
524 16 3 8 2.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCCCNC(=O)OCC3=CC=CC=C3)N
CHEMBL1161825 ghsr_human Human No 8.0 EC50 = 10 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
468 7 2 5 2.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CSC4=CC=CC=C34)N
CHEMBL106841 ghsr_human Human No 8.0 EC50 = 10 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
499 9 5 4 3.6 C1CNCCC1C(=O)NC(CC2=CC3=CC=CC=C3C=C2)C(=O)NC(CC4=CNC5=CC=CC=C54)CO
CHEMBL1162062 ghsr_human Human No 8.0 EC50 = 10 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
523 9 3 6 1.1 C1CS(=O)(=O)C2=CC=CC=C2N(C1=O)CCC(=O)NC(CC3=CC=CC4=CC=CC=C43)C(=O)NCCN
CHEMBL294923 ghsr_human Human No 8.0 EC50 = 10 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
448 7 2 3 4.3 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CCC4=CC=CC=C43)CC2)N
CHEMBL3798645 ghsr_human Human No 8.0 EC50 = 10 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
662 16 6 7 2.8 COC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C(CCCCN)N)C(CC5=CNC6=CC=CC=C65)NC=O
CHEMBL256808 ghsr_human Human No 8.0 EC50 = 10 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
459 6 2 8 3.4 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(S3)C4=CC=CC=N4
CHEMBL482203 ghsr_human Human No 8.0 EC50 = 10 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
432 5 1 6 2.4 CC1=CC=C(O1)C2=CC=C(C=C2)S(=O)(=O)N3CCCCC3C(=O)N4CCC(C4)NC
CHEMBL1161825 ghsr_human Human No 8.0 EC50 = 10 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
468 7 2 5 2.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CSC4=CC=CC=C34)N
CHEMBL294923 ghsr_human Human No 8.0 EC50 = 10 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
448 7 2 3 4.3 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CCC4=CC=CC=C43)CC2)N
CHEMBL488965 ghsr_human Human No 8.0 EC50 = 10 Funct
Agonist activity at GHSRAgonist activity at GHSR
407 7 1 3 4.7 CC(C(=O)N(CC1CCCN1)CC2=CC(=CC=C2)Cl)OC3=CC=CC=C3Cl
CHEMBL248745 ghsr_human Human No 8.0 EC50 = 10 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
499 5 1 8 3.8 CC1CN(CC(N1)(C)C)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC=C(S4)C5=CC=CC=N5)OC
CHEMBL237926 ghsr_human Human No 8.0 EC50 = 10 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
524 16 3 8 2.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCCCNC(=O)OCC3=CC=CC=C3)N
CHEMBL1161825 ghsr_human Human No 8.0 EC50 = 10 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
468 7 2 5 2.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CSC4=CC=CC=C34)N
CHEMBL106841 ghsr_human Human No 8.0 EC50 = 10 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
499 9 5 4 3.6 C1CNCCC1C(=O)NC(CC2=CC3=CC=CC=C3C=C2)C(=O)NC(CC4=CNC5=CC=CC=C54)CO
CHEMBL294923 ghsr_human Human No 8.0 EC50 = 10 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
448 7 2 3 4.3 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CCC4=CC=CC=C43)CC2)N
CHEMBL3798645 ghsr_human Human No 8.0 EC50 = 10 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
662 16 6 7 2.8 COC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C(CCCCN)N)C(CC5=CNC6=CC=CC=C65)NC=O
CHEMBL256808 ghsr_human Human No 8.0 EC50 = 10 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
459 6 2 8 3.4 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(S3)C4=CC=CC=N4
CHEMBL482203 ghsr_human Human No 8.0 EC50 = 10 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
432 5 1 6 2.4 CC1=CC=C(O1)C2=CC=C(C=C2)S(=O)(=O)N3CCCCC3C(=O)N4CCC(C4)NC
CHEMBL105462 ghsr_rat Rat Yes 8.0 EC50 = 10 Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
873 23 11 9 1.9 CC(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CCCCN)C(=O)N)NC(=O)C(CC4=CNC5=CC=CC=C54)NC(=O)C(CC6=CN=CN6)N
CHEMBL2364390 ghsr_human Human No 8.0 EC50 = 10 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
396 4 2 5 4.0 CC1CN(CC(N1)C)C2=CC(=CC=C2)NS(=O)(=O)C3=CC=CC4=CC=CC=C43
CHEMBL2364444 ghsr_human Human No 8.0 EC50 = 10 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
464 5 2 8 4.3 CC1CN(CC(N1)C)C2=CC(=C(C=C2)F)NS(=O)(=O)C3=CC(=C(C=C3)C4=CC=CS4)F
CHEMBL2364343 ghsr_human Human No 8.0 EC50 = 10 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 3 8 2.2 CC1CN(CC(N1)C)C2=CNC(=O)C(=C2)NS(=O)(=O)C3=CC(=C(C=C3)C4=CC=C(O4)C)F
CHEMBL2364479 ghsr_human Human No 8.0 EC50 = 10 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
473 6 2 8 3.4 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CN=C(C=C3)C4=CC(=CS4)C
CHEMBL2364358 ghsr_human Human No 8.0 EC50 = 10 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 6 2 7 3.7 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=NC(=CC=C4)C
CHEMBL2364359 ghsr_human Human No 8.0 EC50 = 10 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
473 6 2 8 3.8 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(S3)C4=NC(=CC=C4)C
CHEMBL2364377 ghsr_human Human No 8.0 EC50 = 10 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
432 5 2 7 3.8 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CSC4=CC=CC=C43
CHEMBL2364477 ghsr_human Human No 8.0 EC50 = 10 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
480 5 2 7 5.2 CC1CN(CC(N1)C)C2=CC(=C(C=C2)Cl)NS(=O)(=O)C3=CC=C(S3)C4=CC=CC=C4F
CHEMBL2364431 ghsr_human Human No 8.0 EC50 = 10 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 2 6 4.6 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=CC4=C3C(=CC=C4)Cl
CHEMBL393531 ghsr_human Human No 8.0 EC50 = 10.1 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
476 11 3 9 -0.7 CC1(CCN(C1)C(=O)OCCN2C(=NN=N2)C(COCC3=CC=CC=C3)NC(=O)C(C)(C)N)O
CHEMBL393531 ghsr_human Human No 8.0 EC50 = 10.1 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
476 11 3 9 -0.7 CC1(CCN(C1)C(=O)OCCN2C(=NN=N2)C(COCC3=CC=CC=C3)NC(=O)C(C)(C)N)O
CHEMBL442151 ghsr_human Human No 7.0 EC50 = 100 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
437 8 2 4 3.4 CC1=CC=CC=C1N2CCN(CC2)C(=O)C(CCCC3=CC=CC=C3)NC(=O)C(C)(C)N
CHEMBL263916 ghsr_human Human No 7.0 EC50 = 100 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
487 7 2 8 4.2 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC(C)C)NS(=O)(=O)C3=CC=C(S3)C4=CC=CC=N4
CHEMBL271948 ghsr_human Human No 7.0 EC50 = 100 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
482 8 2 7 4.2 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)OCC4=CC=CC=C4
CHEMBL410013 ghsr_human Human No 7.0 EC50 = 100 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
447 5 2 8 3.5 CC1CN(CC(N1)C)C2=CC(=C(C=C2)F)NS(=O)(=O)C3=CC=C(S3)C4=CC=CC=N4
CHEMBL473921 ghsr_human Human No 7.0 EC50 = 100 Funct
Agonist activity at human Ghrelin receptorAgonist activity at human Ghrelin receptor
502 6 2 6 4.7 CC1CN(CC(N1)C)CC2=CC=C(C=C2)C3=C(N=CC=C3)C(=O)N4CCC(CC4)NC5=CC=C(C=C5)F
CHEMBL473921 ghsr_human Human No 7.0 EC50 = 100 Funct
Inhibition of human Ghrelin receptorInhibition of human Ghrelin receptor
502 6 2 6 4.7 CC1CN(CC(N1)C)CC2=CC=C(C=C2)C3=C(N=CC=C3)C(=O)N4CCC(CC4)NC5=CC=C(C=C5)F
CHEMBL506986 ghsr_human Human Yes 7.0 EC50 = 100 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 4.3 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CNC5=CC=CC=C54)NC(=O)C(CCCCN)N
CHEMBL3578018 ghsr_human Human No 7.0 EC50 = 100 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
2986 100 42 35 1.6 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=CC5=CC=CC=C54)NC(=O)C(CCCCN)NC(=O)C(CCCCN)NC(=O)CCC(=O)NCC(C(=O)NC(CC(C)C)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC6=CN=CN6)C(=O)NC(CC7=CC=C(C=C7)O)C(=O)NC(CC(C)C)C(=O)NC(CC(=O)N)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(C(C)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC8=CC=C(C=C8)O)C(=O)N)NC(=O)C
CHEMBL3578015 ghsr_human Human No 7.0 EC50 = 100 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
2886 97 41 34 0.9 CC(C)CC(C(=O)NC(CCCNC(=N)N)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)O)C(=O)NC(CC(C)C)C(=O)NC(CC(=O)N)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(C(C)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC3=CC=C(C=C3)O)C(=O)N)NC(=O)C(CCCCNC(=O)CCNC(=O)C(CCC(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC4=CNC5=CC=CC=C54)NC(=O)C(CC6=CC=CC=C6)NC(=O)C(CC7=CC=CC8=CC=CC=C87)NC(=O)C(CCCCN)N)NC(=O)C
CHEMBL473921 ghsr_human Human No 7.0 EC50 = 100 Funct
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
502 6 2 6 4.7 CC1CN(CC(N1)C)CC2=CC=C(C=C2)C3=C(N=CC=C3)C(=O)N4CCC(CC4)NC5=CC=C(C=C5)F
CHEMBL263916 ghsr_human Human No 7.0 EC50 = 100 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
487 7 2 8 4.2 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC(C)C)NS(=O)(=O)C3=CC=C(S3)C4=CC=CC=N4
CHEMBL271948 ghsr_human Human No 7.0 EC50 = 100 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
482 8 2 7 4.2 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)OCC4=CC=CC=C4
CHEMBL410013 ghsr_human Human No 7.0 EC50 = 100 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
447 5 2 8 3.5 CC1CN(CC(N1)C)C2=CC(=C(C=C2)F)NS(=O)(=O)C3=CC=C(S3)C4=CC=CC=N4
CHEMBL473921 ghsr_human Human No 7.0 EC50 = 100 Funct
Agonist activity at human Ghrelin receptorAgonist activity at human Ghrelin receptor
502 6 2 6 4.7 CC1CN(CC(N1)C)CC2=CC=C(C=C2)C3=C(N=CC=C3)C(=O)N4CCC(CC4)NC5=CC=C(C=C5)F
CHEMBL473921 ghsr_human Human No 7.0 EC50 = 100 Funct
Inhibition of human Ghrelin receptorInhibition of human Ghrelin receptor
502 6 2 6 4.7 CC1CN(CC(N1)C)CC2=CC=C(C=C2)C3=C(N=CC=C3)C(=O)N4CCC(CC4)NC5=CC=C(C=C5)F
CHEMBL506986 ghsr_human Human Yes 7.0 EC50 = 100 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 4.3 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CNC5=CC=CC=C54)NC(=O)C(CCCCN)N
CHEMBL3578018 ghsr_human Human No 7.0 EC50 = 100 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
2986 100 42 35 1.6 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=CC5=CC=CC=C54)NC(=O)C(CCCCN)NC(=O)C(CCCCN)NC(=O)CCC(=O)NCC(C(=O)NC(CC(C)C)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC6=CN=CN6)C(=O)NC(CC7=CC=C(C=C7)O)C(=O)NC(CC(C)C)C(=O)NC(CC(=O)N)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(C(C)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC8=CC=C(C=C8)O)C(=O)N)NC(=O)C
CHEMBL3578015 ghsr_human Human No 7.0 EC50 = 100 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
2886 97 41 34 0.9 CC(C)CC(C(=O)NC(CCCNC(=N)N)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)O)C(=O)NC(CC(C)C)C(=O)NC(CC(=O)N)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(C(C)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC3=CC=C(C=C3)O)C(=O)N)NC(=O)C(CCCCNC(=O)CCNC(=O)C(CCC(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC4=CNC5=CC=CC=C54)NC(=O)C(CC6=CC=CC=C6)NC(=O)C(CC7=CC=CC8=CC=CC=C87)NC(=O)C(CCCCN)N)NC(=O)C
CHEMBL2364434 ghsr_human Human No 7.0 EC50 = 100 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
488 6 2 8 4.6 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=C(C=C(C=C4)F)F
CHEMBL2364366 ghsr_human Human No 7.0 EC50 = 100 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 8 3.4 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(S3)C4=CN=CC=C4
CHEMBL2364375 ghsr_human Human No 7.0 EC50 = 100 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 7 3.8 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=CS4)C#N
CHEMBL2364364 ghsr_human Human No 7.0 EC50 = 100 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 3.3 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CN=CC=C4
CHEMBL2364414 ghsr_human Human No 7.0 EC50 = 100 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 8 4.5 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(S3)C4=CC=C(C=C4)F)OC
CHEMBL2364418 ghsr_human Human No 7.0 EC50 = 100 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
438 4 2 5 3.8 CC1CN(CC(N1)C)C2=CC(=C(C=C2)C)NS(=O)(=O)C3=CC=C(C=C3)Br
CHEMBL2364463 ghsr_human Human No 7.0 EC50 = 100 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 5 2 7 3.5 CC1CN(CC(N1)C)C2=CC(=C(C=C2)F)NS(=O)(=O)C3=C(C=C(C=C3)Br)OC
CHEMBL2364397 ghsr_human Human No 7.0 EC50 = 100 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 4.7 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=CC=C4C)OC
CHEMBL2364376 ghsr_human Human No 7.0 EC50 = 100 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
498 8 2 8 4.2 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=CC(=C3)OC4=CC=C(C=C4)OC
CHEMBL519171 ghsr_human Human No 6.0 EC50 = 1000 Funct
Agonist activity at GHSRAgonist activity at GHSR
381 7 2 4 2.7 CC(C(=O)N(CC1CCCN1)C2=CC=CC(=C2)NC(=O)C)OC3=CC=CC=C3
CHEMBL519171 ghsr_human Human No 6.0 EC50 = 1000 Funct
Agonist activity at GHSRAgonist activity at GHSR
381 7 2 4 2.7 CC(C(=O)N(CC1CCCN1)C2=CC=CC(=C2)NC(=O)C)OC3=CC=CC=C3
CHEMBL261497 ghsr_human Human No 7.0 EC50 = 105 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
602 17 4 10 -0.2 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCC3=CC(=CC=C3)S(=O)(=O)CCO)N
CHEMBL261497 ghsr_human Human No 7.0 EC50 = 105 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
602 17 4 10 -0.2 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCC3=CC(=CC=C3)S(=O)(=O)CCO)N
CHEMBL235135 ghsr_human Human No 7.0 EC50 = 107 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
516 13 3 9 1.5 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN(N=N2)CCCC3=CC=CC=C3NS(=O)(=O)C)N
CHEMBL235135 ghsr_human Human No 7.0 EC50 = 107 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
516 13 3 9 1.5 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN(N=N2)CCCC3=CC=CC=C3NS(=O)(=O)C)N
CHEMBL3578018 ghsr_human Human No 7.0 EC50 = 109.6 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
2986 100 42 35 1.6 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=CC5=CC=CC=C54)NC(=O)C(CCCCN)NC(=O)C(CCCCN)NC(=O)CCC(=O)NCC(C(=O)NC(CC(C)C)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC6=CN=CN6)C(=O)NC(CC7=CC=C(C=C7)O)C(=O)NC(CC(C)C)C(=O)NC(CC(=O)N)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(C(C)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC8=CC=C(C=C8)O)C(=O)N)NC(=O)C
CHEMBL374992 ghsr_human Human No 8.0 EC50 = 11 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
535 11 3 4 5.0 CCC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C(C)(C)N)CCC5=CC=CC=C5
CHEMBL374992 ghsr_human Human No 8.0 EC50 = 11 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
535 11 3 4 5.0 CCC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C(C)(C)N)CCC5=CC=CC=C5
CHEMBL2170781 ghsr_human Human Yes 8.0 EC50 = 11.2 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 5.9 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=CC5=CC=CC=C54)NC(=O)C(CCCCN)N
CHEMBL181092 ghsr_human Human No 7.9 EC50 = 11.7 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
510 11 1 5 5.3 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)OC(C)(C)C)C=C(C=C2)OCC3=CC=CC=C3)C(C)C
CHEMBL237058 ghsr_human Human No 6.0 EC50 = 1120 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 6 1.9 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN(N=N2)CC3=CC=CC=C3)N
CHEMBL237058 ghsr_human Human No 6.0 EC50 = 1120 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 6 1.9 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN(N=N2)CC3=CC=CC=C3)N
CHEMBL392522 ghsr_human Human No 6.9 EC50 = 116 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
488 11 3 9 0.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CC3=CC(=CC=C3)NS(=O)(=O)C)N
CHEMBL392522 ghsr_human Human No 6.9 EC50 = 116 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
488 11 3 9 0.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CC3=CC(=CC=C3)NS(=O)(=O)C)N
CHEMBL2170775 ghsr_human Human No 6.9 EC50 = 119.6 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 5.9 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=CC5=CC=CC=C54)NC(=O)C(CCCCN)N
CHEMBL238155 ghsr_human Human No 7.9 EC50 = 12 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
421 10 2 6 2.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CC=CC3=CC=CC=C3)N
CHEMBL240522 ghsr_human Human No 7.9 EC50 = 12 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
566 11 5 6 4.3 COC1=CC=C(C=C1)CN2C(NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CNCCN5)CCC6=CC=CC=C6
CHEMBL385131 ghsr_human Human No 7.9 EC50 = 12 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
535 11 3 4 4.9 CC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C(C)(C)N)CCCC5=CC=CC=C5
CHEMBL252643 ghsr_human Human No 7.9 EC50 = 12 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
596 11 3 5 5.6 COC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5=CC=CC=N5)CCC6=CNC7=CC=CC=C76
CHEMBL238155 ghsr_human Human No 7.9 EC50 = 12 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
421 10 2 6 2.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CC=CC3=CC=CC=C3)N
CHEMBL240522 ghsr_human Human No 7.9 EC50 = 12 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
566 11 5 6 4.3 COC1=CC=C(C=C1)CN2C(NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CNCCN5)CCC6=CC=CC=C6
CHEMBL385131 ghsr_human Human No 7.9 EC50 = 12 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
535 11 3 4 4.9 CC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C(C)(C)N)CCCC5=CC=CC=C5
CHEMBL252643 ghsr_human Human No 7.9 EC50 = 12 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
596 11 3 5 5.6 COC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5=CC=CC=N5)CCC6=CNC7=CC=CC=C76
CHEMBL181108 ghsr_human Human No 7.9 EC50 = 12 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
553 11 2 6 4.5 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)OC(C)(C)C)C=C(C=C2)OC3=CC=CC(=C3)NC(=O)C)C(C)C
CHEMBL2364433 ghsr_human Human No 7.9 EC50 = 12.6 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 3.4 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(C=C3)C4=COC=C4)OC
CHEMBL2364483 ghsr_human Human No 7.9 EC50 = 12.6 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 8 2.7 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=NC=CC=N4
CHEMBL2364387 ghsr_human Human No 7.9 EC50 = 12.6 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 7 2 7 4.5 CCOC1=C(C=C(C=C1)N2CC(NC(C2)C)C)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=CS4
CHEMBL2364336 ghsr_human Human No 7.9 EC50 = 12.6 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
492 6 2 7 5.1 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=C(S4)Cl
CHEMBL2364419 ghsr_human Human No 7.9 EC50 = 12.6 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
448 6 2 8 3.5 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(S3)C4=COC=C4)OC
CHEMBL2364451 ghsr_human Human No 7.9 EC50 = 12.6 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 8 4.2 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC(=C(S3)C4=NC(=CC=C4)C)C
CHEMBL2364458 ghsr_human Human No 7.9 EC50 = 12.6 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 8 3.4 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=NC=CS4
CHEMBL2364486 ghsr_human Human No 7.9 EC50 = 12.6 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 1 7 4.6 CC1CN(CC(N1C)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=CS4
CHEMBL2170779 ghsr_human Human No 7.9 EC50 = 12.6 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
902 25 9 8 4.6 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CC2=CC=CC=C2C=C1)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CNC5=CC=CC=C54)NC(=O)C(CCCCN)N
CHEMBL489403 ghsr_human Human No 6.9 EC50 = 120 Funct
Agonist activity at GHSRAgonist activity at GHSR
393 6 1 3 4.8 CC(C(=O)N(CC1CCCN1)C2=CC=C(C=C2)Cl)OC3=CC(=CC=C3)Cl
CHEMBL528332 ghsr_human Human No 6.9 EC50 = 120 Funct
Agonist activity at GHSRAgonist activity at GHSR
359 6 1 3 4.1 CC(C(=O)N(CC1CCCN1)C2=CC=CC=C2)OC3=CC(=CC=C3)Cl
CHEMBL482623 ghsr_human Human No 6.9 EC50 = 120 Funct
Agonist activity at GHSRAgonist activity at GHSR
387 7 1 3 4.4 CC1=CC(=CC=C1)CN(CC2CCCN2)C(=O)C(C)OC3=CC(=CC=C3)Cl
CHEMBL489403 ghsr_human Human No 6.9 EC50 = 120 Funct
Agonist activity at GHSRAgonist activity at GHSR
393 6 1 3 4.8 CC(C(=O)N(CC1CCCN1)C2=CC=C(C=C2)Cl)OC3=CC(=CC=C3)Cl
CHEMBL528332 ghsr_human Human No 6.9 EC50 = 120 Funct
Agonist activity at GHSRAgonist activity at GHSR
359 6 1 3 4.1 CC(C(=O)N(CC1CCCN1)C2=CC=CC=C2)OC3=CC(=CC=C3)Cl
CHEMBL482623 ghsr_human Human No 6.9 EC50 = 120 Funct
Agonist activity at GHSRAgonist activity at GHSR
387 7 1 3 4.4 CC1=CC(=CC=C1)CN(CC2CCCN2)C(=O)C(C)OC3=CC(=CC=C3)Cl
CHEMBL521612 ghsr_human Human No 5.9 EC50 = 1200 Funct
Agonist activity at GHSRAgonist activity at GHSR
416 7 2 4 3.3 CC(C(=O)N(CC1CCCN1)C2=CC=C(C=C2)NC(=O)C)OC3=CC(=CC=C3)Cl
CHEMBL521612 ghsr_human Human No 5.9 EC50 = 1200 Funct
Agonist activity at GHSRAgonist activity at GHSR
416 7 2 4 3.3 CC(C(=O)N(CC1CCCN1)C2=CC=C(C=C2)NC(=O)C)OC3=CC(=CC=C3)Cl
CHEMBL2170776 ghsr_human Human No 6.9 EC50 = 124.1 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
958 26 9 8 7.6 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=C(C=C3)C(C)(C)C)NC(=O)C(CC4=CC=CC5=CC=CC=C54)NC(=O)C(CCCCN)N
CHEMBL501315 ghsr_rabit Rabbit No 6.9 EC50 = 125.9 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
569 10 2 4 6.5 CC1CN(CC(N1)C)CC2=CC=C(C=C2)C3=CC=CC=C3CN(CCC4=CC(=CC=C4)OC)C(=O)NC5CCCCC5
CHEMBL399704 ghsr_human Human No 6.9 EC50 = 125.9 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
494 4 0 6 4.1 CC1CN(CC(N1C)C)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC(=CC=C4)Br)OC
CHEMBL261466 ghsr_human Human No 6.9 EC50 = 125.9 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
454 5 2 6 3.3 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)Br
CHEMBL501315 ghsr_rabit Rabbit No 6.9 EC50 = 125.9 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
569 10 2 4 6.5 CC1CN(CC(N1)C)CC2=CC=C(C=C2)C3=CC=CC=C3CN(CCC4=CC(=CC=C4)OC)C(=O)NC5CCCCC5
CHEMBL501315 ghsr_human Human No 6.9 EC50 = 125.9 Funct
Agonist activity at GHSR (unknown origin)Agonist activity at GHSR (unknown origin)
569 10 2 4 6.5 CC1CN(CC(N1)C)CC2=CC=C(C=C2)C3=CC=CC=C3CN(CCC4=CC(=CC=C4)OC)C(=O)NC5CCCCC5
CHEMBL399704 ghsr_human Human No 6.9 EC50 = 125.9 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
494 4 0 6 4.1 CC1CN(CC(N1C)C)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC(=CC=C4)Br)OC
CHEMBL261466 ghsr_human Human No 6.9 EC50 = 125.9 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
454 5 2 6 3.3 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)Br
CHEMBL2364357 ghsr_human Human No 6.9 EC50 = 125.9 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 2 7 3.8 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(S3)Br
CHEMBL2364349 ghsr_human Human No 6.9 EC50 = 125.9 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
468 7 2 7 4.3 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(C=C3)OC4=CC=CC=C4)OC
CHEMBL485091 ghsr_human Human No 5.9 EC50 = 1260 Funct
Agonist activity at GHSRAgonist activity at GHSR
359 6 1 3 4.1 CC(C(=O)N(CC1CCCN1)C2=CC=CC=C2Cl)OC3=CC=CC=C3
CHEMBL485091 ghsr_human Human No 5.9 EC50 = 1260 Funct
Agonist activity at GHSRAgonist activity at GHSR
359 6 1 3 4.1 CC(C(=O)N(CC1CCCN1)C2=CC=CC=C2Cl)OC3=CC=CC=C3
CHEMBL330860 ghsr_rat Rat No 7.9 EC50 = 13 Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
543 12 2 4 4.6 CCNC(=O)C(CC1=CC=CC=C1)N(C)C(=O)C(CC2=CC3=CC=CC=C3C=C2)N(C)C(=O)C=CCC(C)(C)N
CHEMBL181627 ghsr_human Human No 7.9 EC50 = 13.1 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
556 13 1 4 6.1 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)CCCC3=CC=CC=C3)C=C(C=C2)OCC4=CC=CC=C4)C(C)C
CHEMBL2170783 ghsr_human Human No 7.9 EC50 = 13.1 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
928 26 9 8 4.8 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(C(C4=CC=CC=C4)C5=CC=CC=C5)NC(=O)C(CCCCN)N
CHEMBL2170779 ghsr_human Human No 7.9 EC50 = 13.4 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 4.6 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CC2=CC=CC=C2C=C1)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CNC5=CC=CC=C54)NC(=O)C(CCCCN)N
CHEMBL403180 ghsr_human Human No 6.9 EC50 = 139 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
462 12 2 7 1.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2C(CCC3=CC=CC=C3)CC#N)N
CHEMBL274599 ghsr_human Human No 7.9 EC50 = 14 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
459 5 3 3 3.7 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CCC5=CC=CC=C54)CC3)N
CHEMBL392076 ghsr_human Human No 7.9 EC50 = 14 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
530 13 2 9 1.2 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC3=CC=CC=C3N(C)S(=O)(=O)C)N
CHEMBL274599 ghsr_human Human No 7.9 EC50 = 14 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
459 5 3 3 3.7 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CCC5=CC=CC=C54)CC3)N
CHEMBL392663 ghsr_human Human No 7.9 EC50 = 14 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
581 11 4 6 5.4 COC1=CC(=C(C=C1)N2C(NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CCNCC5)CCC6=CC=CC=C6)OC
CHEMBL274599 ghsr_human Human No 7.9 EC50 = 14 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
459 5 3 3 3.7 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CCC5=CC=CC=C54)CC3)N
CHEMBL1923617 ghsr_human Human No 7.9 EC50 = 14 Funct
Agonist activity at ghrelin receptor by cell based assayAgonist activity at ghrelin receptor by cell based assay
557 4 3 5 4.8 CCC(C)C1C(=O)N(C(C(=O)NC(C(=O)NCCCC2=CC=CC=C2OCCN1)CC3=CC=C(C=C3)Cl)C)C
CHEMBL392076 ghsr_human Human No 7.9 EC50 = 14 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
530 13 2 9 1.2 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC3=CC=CC=C3N(C)S(=O)(=O)C)N
CHEMBL274599 ghsr_human Human No 7.9 EC50 = 14 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
459 5 3 3 3.7 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CCC5=CC=CC=C54)CC3)N
CHEMBL392663 ghsr_human Human No 7.9 EC50 = 14 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
581 11 4 6 5.4 COC1=CC(=C(C=C1)N2C(NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CCNCC5)CCC6=CC=CC=C6)OC
CHEMBL274599 ghsr_rat Rat No 7.9 EC50 = 14 Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
459 5 3 3 3.7 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CCC5=CC=CC=C54)CC3)N
CHEMBL274599 ghsr_human Human No 7.9 EC50 = 14.1 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
459 5 3 3 3.7 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CCC5=CC=CC=C54)CC3)N
CHEMBL442151 ghsr_human Human No 7.9 EC50 = 14.1 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
437 8 2 4 3.4 CC1=CC=CC=C1N2CCN(CC2)C(=O)C(CCCC3=CC=CC=C3)NC(=O)C(C)(C)N
CHEMBL274599 ghsr_human Human No 7.9 EC50 = 14.1 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
459 5 3 3 3.7 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CCC5=CC=CC=C54)CC3)N
CHEMBL442151 ghsr_human Human No 7.9 EC50 = 14.1 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
437 8 2 4 3.4 CC1=CC=CC=C1N2CCN(CC2)C(=O)C(CCCC3=CC=CC=C3)NC(=O)C(C)(C)N
CHEMBL181247 ghsr_human Human No 7.8 EC50 = 14.4 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
509 10 2 4 4.7 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)NC(C)(C)C)C=C(C=C2)OCC3=CC=CC=C3)C(C)C
CHEMBL393330 ghsr_human Human No 7.8 EC50 = 14.6 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
478 16 4 9 -0.2 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCOC(=O)NCCCCCO)N
CHEMBL393330 ghsr_human Human No 7.8 EC50 = 14.6 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
478 16 4 9 -0.2 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCOC(=O)NCCCCCO)N
CHEMBL411122 ghsr_human Human No 7.8 EC50 = 14.7 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
482 13 3 9 -1.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCNC(=O)CCS(=O)(=O)C)N
CHEMBL411122 ghsr_human Human No 7.8 EC50 = 14.7 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
482 13 3 9 -1.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCNC(=O)CCS(=O)(=O)C)N
CHEMBL483455 ghsr_human Human No 6.9 EC50 = 140 Funct
Agonist activity at GHSRAgonist activity at GHSR
387 7 1 3 4.4 CC1=CC=CC=C1CN(CC2CCCN2)C(=O)C(C)OC3=CC=CC=C3Cl
CHEMBL490627 ghsr_human Human No 6.9 EC50 = 140 Funct
Agonist activity at GHSRAgonist activity at GHSR
416 7 2 4 3.3 CC(C(=O)N(CC1CCCN1)C2=CC=CC(=C2)NC(=O)C)OC3=CC(=CC=C3)Cl
CHEMBL263141 ghsr_human Human No 6.9 EC50 = 140 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
490 16 3 9 -0.5 CCOC(=O)CCNC(=O)CCCN1C(=NN=N1)C(COCC2=CC=CC=C2)NC(=O)C(C)(C)N
CHEMBL375102 ghsr_human Human No 6.9 EC50 = 140 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
613 12 5 4 5.1 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C3=NN=C(N3CCC4=CNC5=CC=CC=C54)CCCC6=CNC7=CC=CC=C76)N
CHEMBL483455 ghsr_human Human No 6.9 EC50 = 140 Funct
Agonist activity at GHSRAgonist activity at GHSR
387 7 1 3 4.4 CC1=CC=CC=C1CN(CC2CCCN2)C(=O)C(C)OC3=CC=CC=C3Cl
CHEMBL490627 ghsr_human Human No 6.9 EC50 = 140 Funct
Agonist activity at GHSRAgonist activity at GHSR
416 7 2 4 3.3 CC(C(=O)N(CC1CCCN1)C2=CC=CC(=C2)NC(=O)C)OC3=CC(=CC=C3)Cl
CHEMBL263141 ghsr_human Human No 6.9 EC50 = 140 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
490 16 3 9 -0.5 CCOC(=O)CCNC(=O)CCCN1C(=NN=N1)C(COCC2=CC=CC=C2)NC(=O)C(C)(C)N
CHEMBL375102 ghsr_human Human No 6.9 EC50 = 140 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
613 12 5 4 5.1 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C3=NN=C(N3CCC4=CNC5=CC=CC=C54)CCCC6=CNC7=CC=CC=C76)N
CHEMBL490390 ghsr_human Human No 4.9 EC50 = 14000 Funct
Agonist activity at GHSRAgonist activity at GHSR
377 8 1 4 3.7 CCC(C(=O)N(CC1CCCN1)C2=CC=C(C=C2)CC#N)OC3=CC=CC=C3
CHEMBL490390 ghsr_human Human No 4.9 EC50 = 14000 Funct
Agonist activity at GHSRAgonist activity at GHSR
377 8 1 4 3.7 CCC(C(=O)N(CC1CCCN1)C2=CC=C(C=C2)CC#N)OC3=CC=CC=C3
CHEMBL239464 ghsr_human Human No 6.8 EC50 = 143 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 5 5 5.1 CCC1=CC=C(C=C1)CN2C(NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CNCCN5)CCC6=CC=CC=C6
CHEMBL239464 ghsr_human Human No 6.9 EC50 = 143 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 5 5 5.1 CCC1=CC=C(C=C1)CN2C(NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CNCCN5)CCC6=CC=CC=C6
CHEMBL237717 ghsr_human Human No 6.8 EC50 = 147 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
514 10 2 9 0.4 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CC3CN(C4=CC=CC=C34)S(=O)(=O)C)N
CHEMBL237717 ghsr_human Human No 6.8 EC50 = 147 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
514 10 2 9 0.4 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CC3CN(C4=CC=CC=C34)S(=O)(=O)C)N
CHEMBL2113327 ghsr_human Human No 7.8 EC50 = 15 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
586 10 4 4 5.6 CCC1=CC=C(C=C1)N2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CCNCC5)CCC6=CNC7=CC=CC=C76
CHEMBL223725 ghsr_human Human No 7.8 EC50 = 15 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
574 12 4 4 5.0 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C3=NN=C(N3CCC4=CC=CC=C4)CCCC5=CNC6=CC=CC=C65)N
CHEMBL2113327 ghsr_human Human No 7.8 EC50 = 15 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
586 10 4 4 5.6 CCC1=CC=C(C=C1)N2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CCNCC5)CCC6=CNC7=CC=CC=C76
CHEMBL223725 ghsr_human Human No 7.8 EC50 = 15 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
574 12 4 4 5.0 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C3=NN=C(N3CCC4=CC=CC=C4)CCCC5=CNC6=CC=CC=C65)N
CHEMBL248746 ghsr_human Human No 7.8 EC50 = 15.9 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
485 5 1 8 3.4 CC1(CN(CCN1)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC=C(S4)C5=CC=CC=N5)OC)C
CHEMBL265950 ghsr_human Human No 7.8 EC50 = 15.9 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
442 6 2 7 2.7 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)N4C=CC=N4
CHEMBL402632 ghsr_human Human No 7.8 EC50 = 15.9 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
459 6 2 8 3.4 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(S3)C4=CC=CC=N4)OC
CHEMBL481014 ghsr_human Human No 7.8 EC50 = 15.9 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 7 1.2 CC1=CC=C(O1)C2=C(C=C(C=C2)S(=O)(=O)N3CCC3C(=O)N4CCC(C4)N)F
CHEMBL481601 ghsr_human Human No 7.8 EC50 = 15.9 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
414 4 1 5 2.4 C1CCN(C(C1)C(=O)N2CCC(C2)N)S(=O)(=O)C3=CC=C(C=C3)C4=CC=CC=C4
CHEMBL248746 ghsr_human Human No 7.8 EC50 = 15.9 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
485 5 1 8 3.4 CC1(CN(CCN1)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC=C(S4)C5=CC=CC=N5)OC)C
CHEMBL265950 ghsr_human Human No 7.8 EC50 = 15.9 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
442 6 2 7 2.7 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)N4C=CC=N4
CHEMBL402632 ghsr_human Human No 7.8 EC50 = 15.9 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
459 6 2 8 3.4 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(S3)C4=CC=CC=N4)OC
CHEMBL481014 ghsr_human Human No 7.8 EC50 = 15.9 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 7 1.2 CC1=CC=C(O1)C2=C(C=C(C=C2)S(=O)(=O)N3CCC3C(=O)N4CCC(C4)N)F
CHEMBL481601 ghsr_human Human No 7.8 EC50 = 15.9 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
414 4 1 5 2.4 C1CCN(C(C1)C(=O)N2CCC(C2)N)S(=O)(=O)C3=CC=C(C=C3)C4=CC=CC=C4
CHEMBL2364346 ghsr_human Human No 7.8 EC50 = 15.9 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
426 5 2 6 4.0 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC4=CC=CC=C4C=C3)OC
CHEMBL2364337 ghsr_human Human No 7.8 EC50 = 15.9 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 8 2.4 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CN=C(C=C3)C4=CC=CO4
CHEMBL2364380 ghsr_human Human No 7.8 EC50 = 15.9 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 4.1 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=CC(=C3)C4=CC=CS4
CHEMBL2364392 ghsr_human Human No 7.8 EC50 = 15.9 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
396 4 2 5 4.0 CC1CN(CC(N1)C)C2=CC(=CC=C2)NS(=O)(=O)C3=CC4=CC=CC=C4C=C3
CHEMBL2364488 ghsr_human Human No 7.8 EC50 = 15.9 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
428 5 3 7 3.1 CC1CN(CC(N1)C)C2=CC(=C(C=C2)O)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=CO4
CHEMBL2364348 ghsr_human Human No 7.8 EC50 = 15.9 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
402 6 2 6 3.2 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C=CC3=CC=CC=C3)OC
CHEMBL2364476 ghsr_human Human No 7.8 EC50 = 15.9 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
478 6 2 9 3.7 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=C(C=C(C(=C3)F)C4=CC=CO4)F
CHEMBL2364368 ghsr_human Human No 7.8 EC50 = 15.9 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 6 2 7 3.7 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(C=C3)C4=NC(=CC=C4)C)OC
CHEMBL2364447 ghsr_human Human No 7.8 EC50 = 15.9 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
448 5 2 8 3.7 CC1CN(CC(N1)C)C2=CC(=C(C=C2)F)NS(=O)(=O)C3=CC(=C(C=C3)C4=COC=C4)F
CHEMBL2364388 ghsr_human Human No 7.8 EC50 = 15.9 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 7 2 7 4.9 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC(C)C)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=CS4
CHEMBL2364360 ghsr_human Human No 7.8 EC50 = 15.9 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 4.0 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=C(C(=CC=C3)Cl)Cl
CHEMBL490601 ghsr_human Human No 6.8 EC50 = 150 Funct
Agonist activity at GHSRAgonist activity at GHSR
373 7 1 3 4.1 CC(C(=O)N(CC1CCCN1)CC2=CC=CC=C2Cl)OC3=CC=CC=C3
CHEMBL402808 ghsr_human Human No 6.8 EC50 = 150 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
462 12 2 7 2.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN(N=N2)C(CCC3=CC=CC=C3)CC#N)N
CHEMBL438154 ghsr_human Human No 6.8 EC50 = 150 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
526 11 2 8 2.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN(N=N2)CCC3=CC4=CC=CC=C4N3S(=O)(=O)C)N
CHEMBL490601 ghsr_human Human No 6.8 EC50 = 150 Funct
Agonist activity at GHSRAgonist activity at GHSR
373 7 1 3 4.1 CC(C(=O)N(CC1CCCN1)CC2=CC=CC=C2Cl)OC3=CC=CC=C3
CHEMBL438154 ghsr_human Human No 6.8 EC50 = 150 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
526 11 2 8 2.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN(N=N2)CCC3=CC4=CC=CC=C4N3S(=O)(=O)C)N
CHEMBL489610 ghsr_human Human No 5.8 EC50 = 1500 Funct
Agonist activity at GHSRAgonist activity at GHSR
373 7 1 3 4.1 CC(C(=O)N(CC1CCCN1)CC2=CC=CC=C2)OC3=CC(=CC=C3)Cl
CHEMBL489610 ghsr_human Human No 5.8 EC50 = 1500 Funct
Agonist activity at GHSRAgonist activity at GHSR
373 7 1 3 4.1 CC(C(=O)N(CC1CCCN1)CC2=CC=CC=C2)OC3=CC(=CC=C3)Cl
CHEMBL235817 ghsr_human Human No 5.8 EC50 = 1520 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 7 0.2 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN(N=N2)CC#N)N
CHEMBL235817 ghsr_human Human No 5.8 EC50 = 1520 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 7 0.2 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN(N=N2)CC#N)N
CHEMBL250973 ghsr_human Human No 6.8 EC50 = 158.5 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
472 6 0 5 4.6 CCOC1=C(C=C(C=C1)CC(=O)N2CCC3=CC(=C(C=C32)N4CC(N(C(C4)C)C)C)OC)Cl
CHEMBL410282 ghsr_human Human No 6.8 EC50 = 158.5 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
452 6 2 6 4.4 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=CC(=C3)C4=CC=CC=C4
CHEMBL1078208 ghsr_human Human No 6.8 EC50 = 158.5 Funct
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
441 7 2 6 3.4 CC(C)OC1=CC=C(C=C1)S(=O)(=O)NC2=CC3=C(CCN(CC3)CC4=CC=NN4)C=C2
CHEMBL250973 ghsr_human Human No 6.8 EC50 = 158.5 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
472 6 0 5 4.6 CCOC1=C(C=C(C=C1)CC(=O)N2CCC3=CC(=C(C=C32)N4CC(N(C(C4)C)C)C)OC)Cl
CHEMBL410282 ghsr_human Human No 6.8 EC50 = 158.5 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
452 6 2 6 4.4 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=CC(=C3)C4=CC=CC=C4
CHEMBL1078208 ghsr_human Human No 6.8 EC50 = 158.5 Funct
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
441 7 2 6 3.4 CC(C)OC1=CC=C(C=C1)S(=O)(=O)NC2=CC3=C(CCN(CC3)CC4=CC=NN4)C=C2
CHEMBL2364371 ghsr_human Human No 6.8 EC50 = 158.5 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 5 2 6 3.4 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC(=CC=C3)Br
CHEMBL2364489 ghsr_human Human No 6.8 EC50 = 158.5 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 6 2 7 3.7 CC1CN(CCN1)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=CS4
CHEMBL403542 ghsr_human Human No 5.8 EC50 = 1580 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
612 12 3 6 5.9 COC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)OC5=CC=CC=N5)CCC6=CNC7=CC=CC=C76
CHEMBL403542 ghsr_human Human No 5.8 EC50 = 1580 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
612 12 3 6 5.9 COC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)OC5=CC=CC=N5)CCC6=CNC7=CC=CC=C76
CHEMBL1078207 ghsr_human Human No 5.8 EC50 = 1584.9 Funct
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
459 6 2 5 4.2 C1CN(CCC2=C1C=CC(=C2)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=CC=C4)CC5=CC=NN5
CHEMBL1078207 ghsr_human Human No 5.8 EC50 = 1584.9 Funct
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
459 6 2 5 4.2 C1CN(CCC2=C1C=CC(=C2)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=CC=C4)CC5=CC=NN5
CHEMBL399651 ghsr_human Human No 7.8 EC50 = 16 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
572 11 2 5 5.8 COC1=CC(=C(C=C1)CN2C(=NN=C2C(C3=CNC4=CC=CC=C43)NC(=O)C5=CC=CC=C5)CCC6=CC=CC=C6)OC
CHEMBL399651 ghsr_human Human No 7.8 EC50 = 16 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
572 11 2 5 5.8 COC1=CC(=C(C=C1)CN2C(=NN=C2C(C3=CNC4=CC=CC=C43)NC(=O)C5=CC=CC=C5)CCC6=CC=CC=C6)OC
CHEMBL275795 ghsr_rat Rat No 7.8 EC50 = 16 Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
491 5 4 5 2.2 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CC3)CC(C5=CC=CC=C5O4)O)N
CHEMBL262889 ghsr_rat Rat No 7.8 EC50 = 16 Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
599 13 2 5 4.6 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)C(CC3=CC=CC=C3)C(=O)NCC4CCCO4)N
CHEMBL417182 ghsr_human Human No 7.8 EC50 = 16.6 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
450 7 2 4 3.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CCC4=CC=CC=C43)CC2)N
CHEMBL417182 ghsr_human Human No 7.8 EC50 = 16.6 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
450 7 2 4 3.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CCC4=CC=CC=C43)CC2)N
CHEMBL417182 ghsr_human Human No 7.8 EC50 = 16.6 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
450 7 2 4 3.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CCC4=CC=CC=C43)CC2)N
CHEMBL1162064 ghsr_human Human No 7.8 EC50 = 17.0 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
594 13 5 5 4.5 C1CNCCC1C(=O)NC(CC2=CC3=CC=CC=C3C=C2)C(=O)NC(CC4=CC5=CC=CC=C5C=C4)C(=O)NCCCCN
CHEMBL2170784 ghsr_human Human No 6.8 EC50 = 161.3 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 4.6 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC5=CC=CC=C5C=C4)NC(=O)C(CCCCN)N
CHEMBL2170697 ghsr_human Human No 6.8 EC50 = 168.6 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
956 27 9 9 4.7 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=C(C=C4)C(=O)C5=CC=CC=C5)NC(=O)C(CCCCN)N
CHEMBL417182 ghsr_human Human No 7.8 EC50 = 17 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
450 7 2 4 3.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CCC4=CC=CC=C43)CC2)N
CHEMBL237933 ghsr_human Human No 7.8 EC50 = 17 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
423 11 2 6 2.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC3=CC=CC=C3)N
CHEMBL1162064 ghsr_human Human No 7.8 EC50 = 17 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
594 13 5 5 4.5 C1CNCCC1C(=O)NC(CC2=CC3=CC=CC=C3C=C2)C(=O)NC(CC4=CC5=CC=CC=C5C=C4)C(=O)NCCCCN
CHEMBL417182 ghsr_human Human No 7.8 EC50 = 17 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
450 7 2 4 3.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CCC4=CC=CC=C43)CC2)N
CHEMBL237933 ghsr_human Human No 7.8 EC50 = 17 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
423 11 2 6 2.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC3=CC=CC=C3)N
CHEMBL1162064 ghsr_human Human No 7.8 EC50 = 17 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
594 13 5 5 4.5 C1CNCCC1C(=O)NC(CC2=CC3=CC=CC=C3C=C2)C(=O)NC(CC4=CC5=CC=CC=C5C=C4)C(=O)NCCCCN
CHEMBL417182 ghsr_human Human No 7.8 EC50 = 17 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
450 7 2 4 3.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CCC4=CC=CC=C43)CC2)N
CHEMBL434609 ghsr_rat Rat No 7.8 EC50 = 17 Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
565 11 2 6 4.4 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)C(CC3=CC(=C(C=C3)F)F)C(=O)NC)N
CHEMBL361612 ghsr_human Human No 7.8 EC50 = 17.8 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
532 10 1 5 5.7 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)C3=CC=CC=C3F)C=C(C=C2)OCC4=CC=CC=C4)C(C)C
CHEMBL2170780 ghsr_human Human No 7.8 EC50 = 17.9 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
902 25 9 8 5.9 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CC=CC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CNC5=CC=CC=C54)NC(=O)C(CCCCN)N
CHEMBL3797639 ghsr_human Human No 6.8 EC50 = 170 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 9 4.6 CC(C)CC(C(=O)NC(CC1=CNC2=CC=CC=C21)C3=NN=C(N3CC4=CC=C(C=C4)OC)C(CC5=CNC6=CC=CC=C65)NC(=O)C(CCCCN)N)C(=O)NC(CC(C)C)C(=O)N
CHEMBL3797639 ghsr_human Human No 6.8 EC50 = 170 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 9 4.6 CC(C)CC(C(=O)NC(CC1=CNC2=CC=CC=C21)C3=NN=C(N3CC4=CC=C(C=C4)OC)C(CC5=CNC6=CC=CC=C65)NC(=O)C(CCCCN)N)C(=O)NC(CC(C)C)C(=O)N
CHEMBL380096 ghsr_human Human No 7.8 EC50 = 18 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
565 12 2 6 3.8 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)CCC3=CC=CC=C3NS(=O)(=O)C)N
CHEMBL611489 ghsr_human Human No 7.8 EC50 = 18 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
486 7 2 7 3.7 CCN(CC)CCN1C2=CC(=CC(=C2C(C1=O)(C3=CC4=CC=CC=C4C=C3)O)C(F)(F)F)C(=O)N
CHEMBL380096 ghsr_human Human No 7.8 EC50 = 18 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
565 12 2 6 3.8 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)CCC3=CC=CC=C3NS(=O)(=O)C)N
CHEMBL376471 ghsr_human Human No 7.8 EC50 = 18 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
590 12 4 5 4.7 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C3=NN=C(N3CC4=CC(=CC=C4)OC)CCCC5=CNC6=CC=CC=C65)N
CHEMBL611489 ghsr_human Human No 7.8 EC50 = 18 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
486 7 2 7 3.7 CCN(CC)CCN1C2=CC(=CC(=C2C(C1=O)(C3=CC4=CC=CC=C4C=C3)O)C(F)(F)F)C(=O)N
CHEMBL380096 ghsr_human Human No 7.8 EC50 = 18 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
565 12 2 6 3.8 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)CCC3=CC=CC=C3NS(=O)(=O)C)N
CHEMBL376471 ghsr_human Human No 7.8 EC50 = 18 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
590 12 4 5 4.7 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C3=NN=C(N3CC4=CC(=CC=C4)OC)CCCC5=CNC6=CC=CC=C65)N
CHEMBL281764 ghsr_rat Rat Yes 7.8 EC50 = 18 Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
529 11 2 4 4.2 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)C(CC3=CC=CC=C3)C(=O)NC)N
CHEMBL380096 ghsr_human Human No 7.7 EC50 = 18.2 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
565 12 2 6 3.8 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)CCC3=CC=CC=C3NS(=O)(=O)C)N
CHEMBL611489 ghsr_human Human No 7.7 EC50 = 18.2 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
486 7 2 7 3.7 CCN(CC)CCN1C2=CC(=CC(=C2C(C1=O)(C3=CC4=CC=CC=C4C=C3)O)C(F)(F)F)C(=O)N
CHEMBL380096 ghsr_human Human No 7.7 EC50 = 18.2 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
565 12 2 6 3.8 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)CCC3=CC=CC=C3NS(=O)(=O)C)N
CHEMBL380096 ghsr_human Human No 7.7 EC50 = 18.2 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
565 12 2 6 3.8 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)CCC3=CC=CC=C3NS(=O)(=O)C)N
CHEMBL489819 ghsr_human Human No 6.8 EC50 = 180 Funct
Agonist activity at GHSRAgonist activity at GHSR
387 7 1 3 4.4 CC1=CC=CC=C1CN(CC2CCCN2)C(=O)C(C)OC3=CC(=CC=C3)Cl
CHEMBL489819 ghsr_human Human No 6.8 EC50 = 180 Funct
Agonist activity at GHSRAgonist activity at GHSR
387 7 1 3 4.4 CC1=CC=CC=C1CN(CC2CCCN2)C(=O)C(C)OC3=CC(=CC=C3)Cl
CHEMBL391859 ghsr_human Human No 6.7 EC50 = 183 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
525 10 4 5 4.5 C1CNCCC1C(=O)NC(CC2=CNC3=CC=CC=C32)C4=NNC(N4CC5=CC=CO5)CCC6=CC=CC=C6
CHEMBL391859 ghsr_human Human No 6.7 EC50 = 183 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
525 10 4 5 4.5 C1CNCCC1C(=O)NC(CC2=CNC3=CC=CC=C32)C4=NNC(N4CC5=CC=CO5)CCC6=CC=CC=C6
CHEMBL2170698 ghsr_human Human No 6.7 EC50 = 183.7 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
928 26 9 8 5.0 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=C(C=C4)C5=CC=CC=C5)NC(=O)C(CCCCN)N
CHEMBL237302 ghsr_human Human No 5.7 EC50 = 1860 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 7 0.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN(N=N2)CCCCC#N)N
CHEMBL237302 ghsr_human Human No 5.7 EC50 = 1860 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 7 0.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN(N=N2)CCCCC#N)N
CHEMBL3578006 ghsr_human Human No 6.7 EC50 = 189.2 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
904 25 10 10 1.4 CC(C)CC(C(=O)NC(CC(=O)N)C(=O)O)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=CC5=CC=CC=C54)NC(=O)C(CCCCN)N
CHEMBL272085 ghsr_human Human No 7.7 EC50 = 19 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 8 1.1 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2C(CC#N)COC3=CC=CC=C3)N
CHEMBL271082 ghsr_human Human No 7.7 EC50 = 19 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
460 11 2 7 2.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN(N=N2)C(CC#N)C=CC3=CC=CC=C3)N
CHEMBL270876 ghsr_human Human No 7.7 EC50 = 19 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
465 12 2 9 0.4 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2C(CC#N)COC3=CC=CC=N3)N
CHEMBL272085 ghsr_human Human No 7.7 EC50 = 19 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 8 1.1 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2C(CC#N)COC3=CC=CC=C3)N
CHEMBL270876 ghsr_human Human No 7.7 EC50 = 19 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
465 12 2 9 0.4 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2C(CC#N)COC3=CC=CC=N3)N
CHEMBL13891 ghsr_rat Rat No 7.7 EC50 = 19 Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
475 5 4 4 2.3 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CC3)CC5=CC=CC=C5C4O)N
CHEMBL415674 ghsr_human Human No 7.7 EC50 = 19.6 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
596 12 5 7 4.2 COC1=CC(=C(C=C1)CN2C(NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CNCCN5)CCC6=CC=CC=C6)OC
CHEMBL415674 ghsr_human Human No 7.7 EC50 = 19.6 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
596 12 5 7 4.2 COC1=CC(=C(C=C1)CN2C(NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CNCCN5)CCC6=CC=CC=C6)OC
CHEMBL182137 ghsr_human Human No 7.7 EC50 = 19.6 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
482 11 1 5 4.4 CCN(CC)CCNC(=O)C1C2=C(CCN1C(=O)OC(C)(C)C)C=C(C=C2)OCC3=CC=CC=C3
CHEMBL434152 ghsr_human Human No 7.7 EC50 = 19.7 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
585 12 2 5 4.9 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)C(C3=CC=CC=C3)NC(=O)C)C=C(C=C2)OCC4=CC=CC=C4)C(C)C
CHEMBL251366 ghsr_human Human No 7.7 EC50 = 20.0 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
479 5 1 7 3.6 CC1CN(CC(N1)C)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC=CC(=C4)C5=CC=CC=N5)OC
CHEMBL270573 ghsr_human Human No 7.7 EC50 = 20.0 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
442 6 2 7 3.5 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=CC(=C3)C4=CC=CO4
CHEMBL1079187 ghsr_human Human No 7.7 EC50 = 20.0 Funct
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
453 8 2 5 4.7 CCCCC1=CC=C(C=C1)S(=O)(=O)NC2=CC3=C(CCN(CC3)CC4=CN=C(N4)C)C=C2
CHEMBL481619 ghsr_human Human No 7.7 EC50 = 20.0 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
457 5 2 6 1.6 C1CCN(C(C1)C(=O)N2CCC(C2)N)S(=O)(=O)C3=CC=C(C=C3)NC(=O)C4=CC=CC=C4
CHEMBL251366 ghsr_human Human No 7.7 EC50 = 20.0 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
479 5 1 7 3.6 CC1CN(CC(N1)C)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC=CC(=C4)C5=CC=CC=N5)OC
CHEMBL270573 ghsr_human Human No 7.7 EC50 = 20.0 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
442 6 2 7 3.5 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=CC(=C3)C4=CC=CO4
CHEMBL1079187 ghsr_human Human No 7.7 EC50 = 20.0 Funct
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
453 8 2 5 4.7 CCCCC1=CC=C(C=C1)S(=O)(=O)NC2=CC3=C(CCN(CC3)CC4=CN=C(N4)C)C=C2
CHEMBL481619 ghsr_human Human No 7.7 EC50 = 20.0 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
457 5 2 6 1.6 C1CCN(C(C1)C(=O)N2CCC(C2)N)S(=O)(=O)C3=CC=C(C=C3)NC(=O)C4=CC=CC=C4
CHEMBL2364443 ghsr_human Human No 7.7 EC50 = 20.0 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 2 7 4.6 CC1CN(CC(N1)C)C2=CC(=C(C=C2)F)NS(=O)(=O)C3=C(C=C(C=C3)C4=CC=CS4)C
CHEMBL2364393 ghsr_human Human No 7.7 EC50 = 20.0 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
414 4 2 5 4.0 CC1CN(CC(N1)C)C2=CC(=CC=C2)NS(=O)(=O)C3=C(C(=CC=C3)Cl)Cl
CHEMBL2364470 ghsr_human Human No 7.7 EC50 = 20.0 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 3.5 CC1CN(CC(N1)C)C2=CC(=CC=C2)NS(=O)(=O)C3=C(C=C(C=C3)C4=CC=CO4)OC
CHEMBL2364440 ghsr_human Human No 7.7 EC50 = 20.0 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
464 5 2 8 4.3 CC1CN(CC(N1)C)C2=CC(=C(C=C2)F)NS(=O)(=O)C3=C(C=C(C=C3)C4=CC=CS4)F
CHEMBL2364435 ghsr_human Human No 7.7 EC50 = 20.0 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
470 6 2 7 4.5 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=CC=C4F
CHEMBL2364373 ghsr_human Human No 7.7 EC50 = 20.0 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 9 3.5 CC1CN(CC(N1)C)C2=CC(=C(C=C2F)OC)NS(=O)(=O)C3=CC=C(S3)C4=CC=CC=N4
CHEMBL2364471 ghsr_human Human No 7.7 EC50 = 20.0 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 4.1 CC1CN(CC(N1)C)C2=CC(=CC=C2)NS(=O)(=O)C3=C(C=C(C=C3)C4=CC=CS4)OC
CHEMBL2364422 ghsr_human Human No 7.7 EC50 = 20.0 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
410 4 2 5 4.4 CC1CN(CC(N1)C)C2=CC(=C(C=C2)C)NS(=O)(=O)C3=CC=CC4=CC=CC=C43
CHEMBL2364465 ghsr_human Human No 7.7 EC50 = 20.0 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 3.2 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=CN4C
CHEMBL2364448 ghsr_human Human No 7.7 EC50 = 20.0 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
464 5 2 7 4.2 CC1CN(CC(N1)C)C2=CC(=C(C=C2)F)NS(=O)(=O)C3=C(C=C(C=C3)C4=COC=C4)Cl
CHEMBL2364404 ghsr_human Human No 7.7 EC50 = 20.0 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
470 6 2 7 4.5 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=C(C=C4)F)OC
CHEMBL2364340 ghsr_human Human No 7.7 EC50 = 20.0 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 8 3.3 CC1CN(CC(N1)C)C2=CC(=NC=C2)NS(=O)(=O)C3=CC(=C(C=C3)C4=CC=C(O4)C)F
CHEMBL182136 ghsr_human Human No 6.7 EC50 = 190 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
481 9 1 4 3.9 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)N(C)C)C=C(C=C2)OCC3=CC=CC=C3)C(C)C
CHEMBL3578006 ghsr_human Human No 6.7 EC50 = 199.5 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
904 25 10 10 1.4 CC(C)CC(C(=O)NC(CC(=O)N)C(=O)O)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=CC5=CC=CC=C54)NC(=O)C(CCCCN)N
CHEMBL3578006 ghsr_human Human No 6.7 EC50 = 199.5 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
904 25 10 10 1.4 CC(C)CC(C(=O)NC(CC(=O)N)C(=O)O)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=CC5=CC=CC=C54)NC(=O)C(CCCCN)N
CHEMBL1161827 ghsr_human Human No 8.7 EC50 = 2 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
482 7 2 5 2.5 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CS(=O)C4=CC=CC=C34)N
CHEMBL295984 ghsr_human Human No 8.7 EC50 = 2 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
544 9 5 5 2.1 CC(C)(C(=O)NC1CCC2=CC=CC=C2N(C1=O)CC3=CC=C(C=C3)C4=CC=CC=C4CNC(=O)NCCO)N
CHEMBL519322 ghsr_human Human No 8.7 EC50 = 2 Funct
Agonist activity at GHSRAgonist activity at GHSR
387 7 1 3 4.4 CC1=CC=CC=C1CN(CC2CCCN2)C(=O)C(C)OC3=CC(=CC=C3)Cl
CHEMBL1161827 ghsr_human Human No 8.7 EC50 = 2 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
482 7 2 5 2.5 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CS(=O)C4=CC=CC=C34)N
CHEMBL295984 ghsr_human Human No 8.7 EC50 = 2 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
544 9 5 5 2.1 CC(C)(C(=O)NC1CCC2=CC=CC=C2N(C1=O)CC3=CC=C(C=C3)C4=CC=CC=C4CNC(=O)NCCO)N
CHEMBL519322 ghsr_human Human No 8.7 EC50 = 2 Funct
Agonist activity at GHSRAgonist activity at GHSR
387 7 1 3 4.4 CC1=CC=CC=C1CN(CC2CCCN2)C(=O)C(C)OC3=CC(=CC=C3)Cl
CHEMBL1161827 ghsr_human Human No 8.7 EC50 = 2 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
482 7 2 5 2.5 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CS(=O)C4=CC=CC=C34)N
CHEMBL295984 ghsr_human Human No 8.7 EC50 = 2 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
544 9 5 5 2.1 CC(C)(C(=O)NC1CCC2=CC=CC=C2N(C1=O)CC3=CC=C(C=C3)C4=CC=CC=C4CNC(=O)NCCO)N
CHEMBL180659 ghsr_human Human No 8.7 EC50 = 2 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
538 12 1 6 4.6 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)OC(C)(C)C(=O)C)C=C(C=C2)OCC3=CC=CC=C3)C(C)C
CHEMBL180659 ghsr_human Human No 8.7 EC50 = 2 Funct
In vivo effective concentration against human growth hormone secretagoguesIn vivo effective concentration against human growth hormone secretagogues
538 12 1 6 4.6 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)OC(C)(C)C(=O)C)C=C(C=C2)OCC3=CC=CC=C3)C(C)C
CHEMBL125498 ghsr_rat Rat No 8.7 EC50 = 2 Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
535 11 2 5 3.9 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)C(CC3=CC=CS3)C(=O)NC)N
CHEMBL1161824 ghsr_human Human No 8.7 EC50 = 2.1 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
509 5 3 5 2.1 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CC3)CS(=O)(=O)C5=CC=CC=C45)N
CHEMBL1161824 ghsr_human Human No 8.7 EC50 = 2.1 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
509 5 3 5 2.1 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CC3)CS(=O)(=O)C5=CC=CC=C45)N
CHEMBL1161824 ghsr_human Human No 8.7 EC50 = 2.1 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
509 5 3 5 2.1 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CC3)CS(=O)(=O)C5=CC=CC=C45)N
CHEMBL1161824 ghsr_human Human No 8.7 EC50 = 2.1 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
509 5 3 5 2.1 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CC3)CS(=O)(=O)C5=CC=CC=C45)N
CHEMBL1161824 ghsr_human Human No 8.7 EC50 = 2.1 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
509 5 3 5 2.1 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CC3)CS(=O)(=O)C5=CC=CC=C45)N
CHEMBL1161824 ghsr_human Human No 8.7 EC50 = 2.1 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
509 5 3 5 2.1 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CC3)CS(=O)(=O)C5=CC=CC=C45)N
CHEMBL181832 ghsr_human Human No 8.7 EC50 = 2.1 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
558 12 1 5 5.5 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)CC3=CC=CC=C3OC)C=C(C=C2)OCC4=CC=CC=C4)C(C)C
CHEMBL2170695 ghsr_human Human No 8.7 EC50 = 2.1 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
919 25 8 9 6.8 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CSC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=CC5=CC=CC=C54)NC(=O)C(CCCCN)N
CHEMBL33182 ghsr_human Human No 8.6 EC50 = 2.3 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
560 12 4 9 -0.1 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCN(CC2)C3=CC=CC=C3NS(=O)(=O)CC(=O)O)N
CHEMBL33182 ghsr_human Human No 8.6 EC50 = 2.3 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
560 12 4 9 -0.1 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCN(CC2)C3=CC=CC=C3NS(=O)(=O)CC(=O)O)N
CHEMBL33182 ghsr_human Human No 8.6 EC50 = 2.3 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
560 12 4 9 -0.1 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCN(CC2)C3=CC=CC=C3NS(=O)(=O)CC(=O)O)N
CHEMBL2113326 ghsr_human Human No 8.6 EC50 = 2.3 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
558 9 4 4 4.8 C1CNCCC1C(=O)NC(CC2=CNC3=CC=CC=C32)C4=NN=C(N4C5=CC=CC=C5)CCC6=CNC7=CC=CC=C76
CHEMBL2113326 ghsr_human Human No 8.6 EC50 = 2.3 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
558 9 4 4 4.8 C1CNCCC1C(=O)NC(CC2=CNC3=CC=CC=C32)C4=NN=C(N4C5=CC=CC=C5)CCC6=CNC7=CC=CC=C76
CHEMBL181786 ghsr_human Human No 8.6 EC50 = 2.3 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
564 10 1 8 6.2 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)OC(C)(C)C)C=C(C=C2)OC3=CC=C(C=C3)C(F)(F)F)C(C)C
CHEMBL182158 ghsr_human Human No 8.6 EC50 = 2.4 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
542 11 1 6 5.9 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)OC(C)(C)C)C=C(C=C2)OC3=CC=C(C=C3)SC)C(C)C
CHEMBL241775 ghsr_human Human No 8.6 EC50 = 2.5 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
602 11 4 5 4.7 COC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CCCNC5)CCC6=CNC7=CC=CC=C76
CHEMBL241775 ghsr_human Human No 8.6 EC50 = 2.5 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
602 11 4 5 4.7 COC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CCCNC5)CCC6=CNC7=CC=CC=C76
CHEMBL1161827 ghsr_human Human No 8.6 EC50 = 2.5 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
482 7 2 5 2.5 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CS(=O)C4=CC=CC=C34)N
CHEMBL1161827 ghsr_human Human No 8.6 EC50 = 2.5 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
482 7 2 5 2.5 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CS(=O)C4=CC=CC=C34)N
CHEMBL251573 ghsr_human Human No 8.6 EC50 = 2.5 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
475 5 1 9 3.1 CC1CN(CC(N1)C)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC=C(S4)C5=NOC=C5)OC
CHEMBL251573 ghsr_human Human No 8.6 EC50 = 2.5 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
475 5 1 9 3.1 CC1CN(CC(N1)C)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC=C(S4)C5=NOC=C5)OC
CHEMBL1161827 ghsr_human Human No 8.6 EC50 = 2.5 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
482 7 2 5 2.5 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CS(=O)C4=CC=CC=C34)N
CHEMBL272540 ghsr_human Human No 8.6 EC50 = 2.5 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
449 6 2 9 2.9 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(S3)C4=CN=CO4
CHEMBL272540 ghsr_human Human No 8.6 EC50 = 2.5 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
449 6 2 9 2.9 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(S3)C4=CN=CO4
CHEMBL480639 ghsr_human Human No 8.6 EC50 = 2.5 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
464 4 1 7 2.9 CC1CN(CC(N1)C)C(=O)C2CCCCN2S(=O)(=O)C3=CC(=C(C=C3)C4=CC=C(O4)C)F
CHEMBL480639 ghsr_human Human No 8.6 EC50 = 2.5 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
464 4 1 7 2.9 CC1CN(CC(N1)C)C(=O)C2CCCCN2S(=O)(=O)C3=CC(=C(C=C3)C4=CC=C(O4)C)F
CHEMBL2364481 ghsr_human Human No 8.6 EC50 = 2.5 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
490 6 2 8 4.6 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=C(C=C(C=C3)C4=CSC(=C4)C)F
CHEMBL2364402 ghsr_human Human No 8.6 EC50 = 2.5 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 8 4.2 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=C(C=C(C=C3)C4=CC=CS4)F)OC
CHEMBL2364415 ghsr_human Human No 8.6 EC50 = 2.5 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
492 6 2 7 5.1 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(S3)C4=CC=CC=C4Cl
CHEMBL2364379 ghsr_human Human No 8.6 EC50 = 2.5 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 4.1 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(C=C3)C4=CSC=C4)OC
CHEMBL2364428 ghsr_human Human No 8.6 EC50 = 2.5 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 6 5.0 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CC(=CC=C4)Cl
CHEMBL1161829 ghsr_human Human No 8.6 EC50 = 2.7 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
450 7 2 4 3.4 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CC2)COC4=CC=CC=C34)N
CHEMBL1161829 ghsr_human Human No 8.6 EC50 = 2.7 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
450 7 2 4 3.4 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CC2)COC4=CC=CC=C34)N
CHEMBL1161829 ghsr_human Human No 8.6 EC50 = 2.7 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
450 7 2 4 3.4 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CC2)COC4=CC=CC=C34)N
CHEMBL1161829 ghsr_human Human No 8.6 EC50 = 2.7 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
450 7 2 4 3.4 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CC2)COC4=CC=CC=C34)N
CHEMBL1161829 ghsr_human Human No 8.6 EC50 = 2.7 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
450 7 2 4 3.4 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CC2)COC4=CC=CC=C34)N
CHEMBL1161829 ghsr_human Human No 8.6 EC50 = 2.7 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
450 7 2 4 3.4 CC(C)(C(=O)NC(CCCC1=CC=CC=C1)C(=O)N2CCC3(CC2)COC4=CC=CC=C34)N
CHEMBL432461 ghsr_human Human No 8.6 EC50 = 2.8 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
544 11 3 7 2.8 CC(C)S(=O)(=O)NC1=CC=CC=C1N2CCN(CC2)C(=O)C(CCCC3=CC=CC=C3)NC(=O)C(C)(C)N
CHEMBL432461 ghsr_human Human No 8.6 EC50 = 2.8 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
544 11 3 7 2.8 CC(C)S(=O)(=O)NC1=CC=CC=C1N2CCN(CC2)C(=O)C(CCCC3=CC=CC=C3)NC(=O)C(C)(C)N
CHEMBL2170781 ghsr_human Human Yes 8.6 EC50 = 2.8 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 5.9 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=CC5=CC=CC=C54)NC(=O)C(CCCCN)N
CHEMBL432461 ghsr_human Human No 8.6 EC50 = 2.8 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
544 11 3 7 2.8 CC(C)S(=O)(=O)NC1=CC=CC=C1N2CCN(CC2)C(=O)C(CCCC3=CC=CC=C3)NC(=O)C(C)(C)N
CHEMBL274340 ghsr_rat Rat No 8.5 EC50 = 2.9 Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
475 5 3 4 3.3 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCCC4(C3)CCC5=CC=CC=C5O4)N
CHEMBL485090 ghsr_human Human No 7.7 EC50 = 20 Funct
Agonist activity at GHSRAgonist activity at GHSR
407 7 1 3 4.7 CC(C(=O)N(CC1CCCN1)CC2=CC(=CC=C2)Cl)OC3=CC(=CC=C3)Cl
CHEMBL491221 ghsr_human Human No 7.7 EC50 = 20 Funct
Agonist activity at GHSRAgonist activity at GHSR
373 7 1 3 4.1 CC(C(=O)N(CC1CCCN1)CC2=CC=CC=C2)OC3=CC=CC=C3Cl
CHEMBL491044 ghsr_human Human No 7.7 EC50 = 20 Funct
Agonist activity at GHSRAgonist activity at GHSR
416 7 2 4 3.3 CC(C(=O)N(CC1CCCN1)C2=CC=C(C=C2)NC(=O)C)OC3=CC(=CC=C3)Cl
CHEMBL235793 ghsr_human Human No 7.7 EC50 = 20 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
453 11 2 8 1.5 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2C(C3=CC=CC=C3)C(=O)OC)N
CHEMBL3799222 ghsr_human Human No 7.7 EC50 = 20 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
790 21 6 9 4.5 CC(C)CC(C(=O)NC(CC1=CNC2=CC=CC=C21)C3=NN=C(N3CC4=CC=C(C=C4)OC)C(CC5=CNC6=CC=CC=C65)NC(=O)C(CCCCN)N)C(=O)OC
CHEMBL485090 ghsr_human Human No 7.7 EC50 = 20 Funct
Agonist activity at GHSRAgonist activity at GHSR
407 7 1 3 4.7 CC(C(=O)N(CC1CCCN1)CC2=CC(=CC=C2)Cl)OC3=CC(=CC=C3)Cl
CHEMBL491221 ghsr_human Human No 7.7 EC50 = 20 Funct
Agonist activity at GHSRAgonist activity at GHSR
373 7 1 3 4.1 CC(C(=O)N(CC1CCCN1)CC2=CC=CC=C2)OC3=CC=CC=C3Cl
CHEMBL491044 ghsr_human Human No 7.7 EC50 = 20 Funct
Agonist activity at GHSRAgonist activity at GHSR
416 7 2 4 3.3 CC(C(=O)N(CC1CCCN1)C2=CC=C(C=C2)NC(=O)C)OC3=CC(=CC=C3)Cl
CHEMBL235793 ghsr_human Human No 7.7 EC50 = 20 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
453 11 2 8 1.5 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2C(C3=CC=CC=C3)C(=O)OC)N
CHEMBL3799222 ghsr_human Human No 7.7 EC50 = 20 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
790 21 6 9 4.5 CC(C)CC(C(=O)NC(CC1=CNC2=CC=CC=C21)C3=NN=C(N3CC4=CC=C(C=C4)OC)C(CC5=CNC6=CC=CC=C65)NC(=O)C(CCCCN)N)C(=O)OC
CHEMBL13383 ghsr_rat Rat No 7.7 EC50 = 20 Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
473 5 3 4 2.7 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCCC4(C3)CC5=CC=CC=C5C4=O)N
CHEMBL332414 ghsr_rat Rat No 7.7 EC50 = 20 Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
655 11 2 4 4.9 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)C(CC3=CC=C(C=C3)I)C(=O)NC)N
CHEMBL362798 ghsr_human Human No 7.7 EC50 = 20.9 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
508 11 1 4 5.6 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)CC(C)(C)C)C=C(C=C2)OCC3=CC=CC=C3)C(C)C
CHEMBL490009 ghsr_human Human No 6.7 EC50 = 200 Funct
Agonist activity at GHSRAgonist activity at GHSR
416 7 2 4 3.3 CC(C(=O)N(CC1CCCN1)C2=CC=CC(=C2)NC(=O)C)OC3=CC=CC=C3Cl
CHEMBL235012 ghsr_human Human No 6.7 EC50 = 200 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 9 3 7 0.3 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C3=NN=NN3CCC(=O)OC)N
CHEMBL490009 ghsr_human Human No 6.7 EC50 = 200 Funct
Agonist activity at GHSRAgonist activity at GHSR
416 7 2 4 3.3 CC(C(=O)N(CC1CCCN1)C2=CC=CC(=C2)NC(=O)C)OC3=CC=CC=C3Cl
CHEMBL235012 ghsr_human Human No 6.7 EC50 = 200 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 9 3 7 0.3 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C3=NN=NN3CCC(=O)OC)N
CHEMBL489794 ghsr_human Human No 5.7 EC50 = 2000 Funct
Agonist activity at GHSRAgonist activity at GHSR
371 7 1 4 4.0 CC(C(=O)N(CC1CCCN1)C2=CC(=CC=C2)SC)OC3=CC=CC=C3
CHEMBL491835 ghsr_human Human No 5.7 EC50 = 2000 Funct
Agonist activity at GHSRAgonist activity at GHSR
367 7 2 4 2.3 CC(=O)NC1=CC=C(C=C1)N(CC2CCCN2)C(=O)COC3=CC=CC=C3
CHEMBL519196 ghsr_human Human No 5.7 EC50 = 2000 Funct
Agonist activity at GHSRAgonist activity at GHSR
445 9 1 4 5.6 CCC(C(=O)N(CC1CCCN1)C2=CC=CC(=C2OC)C3=CC=CC=C3)OC4=CC=CC=C4
CHEMBL489794 ghsr_human Human No 5.7 EC50 = 2000 Funct
Agonist activity at GHSRAgonist activity at GHSR
371 7 1 4 4.0 CC(C(=O)N(CC1CCCN1)C2=CC(=CC=C2)SC)OC3=CC=CC=C3
CHEMBL491835 ghsr_human Human No 5.7 EC50 = 2000 Funct
Agonist activity at GHSRAgonist activity at GHSR
367 7 2 4 2.3 CC(=O)NC1=CC=C(C=C1)N(CC2CCCN2)C(=O)COC3=CC=CC=C3
CHEMBL519196 ghsr_human Human No 5.7 EC50 = 2000 Funct
Agonist activity at GHSRAgonist activity at GHSR
445 9 1 4 5.6 CCC(C(=O)N(CC1CCCN1)C2=CC=CC(=C2OC)C3=CC=CC=C3)OC4=CC=CC=C4
CHEMBL271082 ghsr_human Human No 6.7 EC50 = 202 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
460 11 2 7 2.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN(N=N2)C(CC#N)C=CC3=CC=CC=C3)N
CHEMBL271082 ghsr_human Human No 6.7 EC50 = 202 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
460 11 2 7 2.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN(N=N2)C(CC#N)C=CC3=CC=CC=C3)N
CHEMBL409258 ghsr_human Human No 6.7 EC50 = 204 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
462 14 4 9 -3.5 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCC(=O)O)N
CHEMBL409258 ghsr_human Human No 6.7 EC50 = 204 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
462 14 4 9 -3.5 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCC(=O)O)N
CHEMBL181337 ghsr_human Human No 7.7 EC50 = 21 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
545 11 1 7 3.5 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)S(=O)(=O)N(C)C)C=C(C=C2)OCC3=CC=CC=C3)C(C)C
CHEMBL181352 ghsr_human Human No 7.7 EC50 = 21 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
578 11 1 6 5.1 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)S(=O)(=O)C3=CC=CC=C3)C=C(C=C2)OCC4=CC=CC=C4)C(C)C
CHEMBL332987 ghsr_rat Rat No 7.7 EC50 = 21 Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
599 13 2 5 4.6 CC(C)(CC=CC(=O)N(C)C(CC1=CC=CC2=CC=CC=C21)C(=O)N(C)C(CC3=CC=CC=C3)C(=O)NCC4CCCO4)N
CHEMBL49884 ghsr_human Human No 7.7 EC50 = 21.9 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
434 6 2 3 3.9 CC(C)(C(=O)NC(CCC1=CC=CC=C1)C(=O)N2CCC3(CCC4=CC=CC=C43)CC2)N
CHEMBL49884 ghsr_human Human No 7.7 EC50 = 21.9 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
434 6 2 3 3.9 CC(C)(C(=O)NC(CCC1=CC=CC=C1)C(=O)N2CCC3(CCC4=CC=CC=C43)CC2)N
CHEMBL49884 ghsr_human Human No 7.7 EC50 = 21.9 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
434 6 2 3 3.9 CC(C)(C(=O)NC(CCC1=CC=CC=C1)C(=O)N2CCC3(CCC4=CC=CC=C43)CC2)N
CHEMBL49884 ghsr_human Human No 7.7 EC50 = 21.9 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
434 6 2 3 3.9 CC(C)(C(=O)NC(CCC1=CC=CC=C1)C(=O)N2CCC3(CCC4=CC=CC=C43)CC2)N
CHEMBL376736 ghsr_human Human No 6.7 EC50 = 210 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
564 10 4 5 4.4 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C3=NN=C(N3CC4=CC=C(C=C4)F)CCC5=CNC6=CC=CC=C65)N
CHEMBL376736 ghsr_human Human No 6.7 EC50 = 210 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
564 10 4 5 4.4 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C3=NN=C(N3CC4=CC=C(C=C4)F)CCC5=CNC6=CC=CC=C65)N
CHEMBL178502 ghsr_human Human No 6.7 EC50 = 219 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
468 10 2 5 4.0 CC(C)NCCNC(=O)C1C2=C(CCN1C(=O)OC(C)(C)C)C=C(C=C2)OCC3=CC=CC=C3
CHEMBL49884 ghsr_human Human No 7.7 EC50 = 22 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
434 6 2 3 3.9 CC(C)(C(=O)NC(CCC1=CC=CC=C1)C(=O)N2CCC3(CCC4=CC=CC=C43)CC2)N
CHEMBL402086 ghsr_human Human No 7.7 EC50 = 22 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
448 11 2 7 1.4 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CC(CC3=CC=CC=C3)C#N)N
CHEMBL49884 ghsr_human Human No 7.7 EC50 = 22 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
434 6 2 3 3.9 CC(C)(C(=O)NC(CCC1=CC=CC=C1)C(=O)N2CCC3(CCC4=CC=CC=C43)CC2)N
CHEMBL402086 ghsr_human Human No 7.7 EC50 = 22 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
448 11 2 7 1.4 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CC(CC3=CC=CC=C3)C#N)N
CHEMBL492028 ghsr_human Human No 6.7 EC50 = 220 Funct
Agonist activity at GHSRAgonist activity at GHSR
373 7 1 3 4.1 CC(C(=O)N(CC1CCCN1)CC2=CC=C(C=C2)Cl)OC3=CC=CC=C3
CHEMBL492028 ghsr_human Human No 6.7 EC50 = 220 Funct
Agonist activity at GHSRAgonist activity at GHSR
373 7 1 3 4.1 CC(C(=O)N(CC1CCCN1)CC2=CC=C(C=C2)Cl)OC3=CC=CC=C3
CHEMBL409327 ghsr_human Human No 7.6 EC50 = 23 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
494 14 3 7 1.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCC3=CC=CC=C3)N
CHEMBL410060 ghsr_human Human No 7.6 EC50 = 23 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
480 12 3 9 0.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2C(CC#N)COC3=CC=CC=C3O)N
CHEMBL266199 ghsr_human Human No 7.6 EC50 = 23 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
497 10 3 5 3.3 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C3=NN=C(N3CC4=CC=CO4)CCC5=CC=CC=C5)N
CHEMBL409327 ghsr_human Human No 7.6 EC50 = 23 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
494 14 3 7 1.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCC3=CC=CC=C3)N
CHEMBL410060 ghsr_human Human No 7.6 EC50 = 23 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
480 12 3 9 0.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2C(CC#N)COC3=CC=CC=C3O)N
CHEMBL266199 ghsr_human Human No 7.6 EC50 = 23 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
497 10 3 5 3.3 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C3=NN=C(N3CC4=CC=CO4)CCC5=CC=CC=C5)N
CHEMBL2170781 ghsr_human Human Yes 6.6 EC50 = 237.6 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 5.9 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=CC5=CC=CC=C54)NC(=O)C(CCCCN)N
CHEMBL403426 ghsr_human Human No 7.6 EC50 = 24 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
619 12 3 6 5.4 COC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)OC5CCOCC5)CCC6=CNC7=CC=CC=C76
CHEMBL251855 ghsr_human Human No 7.6 EC50 = 24 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
619 12 3 6 5.4 COC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)OC5CCOCC5)CCC6=CNC7=CC=CC=C76
CHEMBL403426 ghsr_human Human No 7.6 EC50 = 24 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
619 12 3 6 5.4 COC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)OC5CCOCC5)CCC6=CNC7=CC=CC=C76
CHEMBL251855 ghsr_human Human No 7.6 EC50 = 24 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
619 12 3 6 5.4 COC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)OC5CCOCC5)CCC6=CNC7=CC=CC=C76
CHEMBL122420 ghsr_rat Rat No 7.6 EC50 = 24 Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
529 11 2 4 4.2 CC(C)(CC=CC(=O)N(C)C(CC1=CC=CC2=CC=CC=C21)C(=O)N(C)C(CC3=CC=CC=C3)C(=O)NC)N
CHEMBL2170699 ghsr_human Human No 6.6 EC50 = 240.9 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
852 25 9 8 3.3 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=CC=C4)NC(=O)C(CCCCN)N
CHEMBL402808 ghsr_human Human No 6.6 EC50 = 244 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
462 12 2 7 2.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN(N=N2)C(CCC3=CC=CC=C3)CC#N)N
CHEMBL402808 ghsr_human Human No 6.6 EC50 = 244 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
462 12 2 7 2.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN(N=N2)C(CCC3=CC=CC=C3)CC#N)N
CHEMBL404227 ghsr_human Human No 5.6 EC50 = 2470 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
448 11 2 7 1.9 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN(N=N2)CC(CC3=CC=CC=C3)C#N)N
CHEMBL404227 ghsr_human Human No 5.6 EC50 = 2470 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
448 11 2 7 1.9 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN(N=N2)CC(CC3=CC=CC=C3)C#N)N
CHEMBL13930 ghsr_rat Rat No 7.6 EC50 = 25 Funct
In vitro growth hormone release was determined in rat pituitary cell assayIn vitro growth hormone release was determined in rat pituitary cell assay
475 5 3 4 3.3 CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)N3CCC4(CCC5=CC=CC=C5O4)CC3)N
CHEMBL2364383 ghsr_human Human No 7.6 EC50 = 25.1 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 3 8 3.1 CC1CN(CC(N1)C)C2=CC(=C(C=C2)O)NS(=O)(=O)C3=CC=C(S3)C4=CC=CC=N4
CHEMBL2364396 ghsr_human Human No 7.6 EC50 = 25.1 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
462 5 2 6 5.1 CC1CN(CC(N1)C)C2=CC(=CC=C2)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=C(S4)Cl
CHEMBL2364412 ghsr_human Human No 7.6 EC50 = 25.1 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 5.2 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(S3)C4=C(C=CC=C4C)C)OC
CHEMBL2364344 ghsr_human Human No 7.6 EC50 = 25.1 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 8 3.7 CC1CN(CC(N1)C)C2=NC(=C(C=C2)OC)NS(=O)(=O)C3=C(C=C(C=C3)C4=COC=C4)Cl
CHEMBL2364452 ghsr_human Human No 7.6 EC50 = 25.1 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 10 3.0 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(S3)C4=CSN=N4
CHEMBL2364445 ghsr_human Human No 7.6 EC50 = 25.1 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
430 5 2 7 3.6 CC1CN(CC(N1)C)C2=CC(=C(C=C2)F)NS(=O)(=O)C3=CC=C(C=C3)C4=COC=C4
CHEMBL2364369 ghsr_human Human No 7.6 EC50 = 25.1 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 5 2 7 4.7 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC4=C(S3)C=CC(=C4)Cl
CHEMBL2364421 ghsr_human Human No 7.6 EC50 = 25.1 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
478 6 2 8 4.5 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(S3)C4=CC=C(S4)C
CHEMBL2364400 ghsr_human Human No 7.6 EC50 = 25.1 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
412 5 2 6 2.7 CC1CN(CC(N1)C)C2=CC(=CC=C2)NS(=O)(=O)C3=CC=C(C=C3)N4C=CC=N4
CHEMBL2364410 ghsr_human Human No 7.6 EC50 = 25.1 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 4.8 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(S3)C4=CC=CC=C4C
CHEMBL507551 ghsr_human Human No 6.6 EC50 = 250 Funct
Agonist activity at GHSRAgonist activity at GHSR
393 6 1 3 4.8 CC(C(=O)N(CC1CCCN1)C2=CC(=CC=C2)Cl)OC3=CC=CC=C3Cl
CHEMBL507551 ghsr_human Human No 6.6 EC50 = 250 Funct
Agonist activity at GHSRAgonist activity at GHSR
393 6 1 3 4.8 CC(C(=O)N(CC1CCCN1)C2=CC(=CC=C2)Cl)OC3=CC=CC=C3Cl
CHEMBL3578014 ghsr_human Human No 6.6 EC50 = 251.2 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
2915 99 41 34 1.6 CC(C)CC(C(=O)NC(CCCNC(=N)N)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)O)C(=O)NC(CC(C)C)C(=O)NC(CC(=O)N)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(C(C)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC3=CC=C(C=C3)O)C(=O)N)NC(=O)C(CCCCNC(=O)CCCCCNC(=O)C(CC(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC4=CNC5=CC=CC=C54)NC(=O)C(CC6=CC=CC=C6)NC(=O)C(CC7=CC=CC8=CC=CC=C87)NC(=O)C(CCCCN)N)NC(=O)C
CHEMBL3578014 ghsr_human Human No 6.6 EC50 = 251.2 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
2915 99 41 34 1.6 CC(C)CC(C(=O)NC(CCCNC(=N)N)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)O)C(=O)NC(CC(C)C)C(=O)NC(CC(=O)N)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(C(C)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC3=CC=C(C=C3)O)C(=O)N)NC(=O)C(CCCCNC(=O)CCCCCNC(=O)C(CC(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC4=CNC5=CC=CC=C54)NC(=O)C(CC6=CC=CC=C6)NC(=O)C(CC7=CC=CC8=CC=CC=C87)NC(=O)C(CCCCN)N)NC(=O)C
CHEMBL241242 ghsr_human Human No 6.6 EC50 = 256 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
525 12 4 5 4.3 COC1=CC=C(C=C1)CN2C(NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)CCN)CCC5=CC=CC=C5
CHEMBL241242 ghsr_human Human No 6.6 EC50 = 256 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
525 12 4 5 4.3 COC1=CC=C(C=C1)CN2C(NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)CCN)CCC5=CC=CC=C5
CHEMBL181051 ghsr_human Human No 6.6 EC50 = 257 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
452 9 1 4 3.9 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)C)C=C(C=C2)OCC3=CC=CC=C3)C(C)C
CHEMBL369571 ghsr_human Human No 6.6 EC50 = 257 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
468 9 2 5 3.9 CC(C)(C)OC(=O)N1CCC2=C(C1C(=O)NCC(C)(C)CN)C=CC(=C2)OCC3=CC=CC=C3
CHEMBL237059 ghsr_human Human No 6.6 EC50 = 259 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
488 11 3 9 0.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CC3=CC=C(C=C3)NS(=O)(=O)C)N
CHEMBL237059 ghsr_human Human No 6.6 EC50 = 259 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
488 11 3 9 0.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CC3=CC=C(C=C3)NS(=O)(=O)C)N
CHEMBL410499 ghsr_human Human No 7.6 EC50 = 26 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 10 0.4 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCC(F)(F)F)N
CHEMBL410499 ghsr_human Human No 7.6 EC50 = 26 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 10 0.4 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCC(F)(F)F)N
CHEMBL366916 ghsr_human Human No 7.6 EC50 = 26.7 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
542 12 1 4 5.8 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)CCC3=CC=CC=C3)C=C(C=C2)OCC4=CC=CC=C4)C(C)C
CHEMBL488966 ghsr_human Human No 6.6 EC50 = 260 Funct
Agonist activity at GHSRAgonist activity at GHSR
407 7 1 3 4.7 CC(C(=O)N(CC1CCCN1)CC2=CC=CC=C2Cl)OC3=CC=CC=C3Cl
CHEMBL488966 ghsr_human Human No 6.6 EC50 = 260 Funct
Agonist activity at GHSRAgonist activity at GHSR
407 7 1 3 4.7 CC(C(=O)N(CC1CCCN1)CC2=CC=CC=C2Cl)OC3=CC=CC=C3Cl
CHEMBL3578014 ghsr_human Human No 6.6 EC50 = 266.8 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
2915 99 41 34 1.6 CC(C)CC(C(=O)NC(CCCNC(=N)N)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)O)C(=O)NC(CC(C)C)C(=O)NC(CC(=O)N)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(C(C)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC3=CC=C(C=C3)O)C(=O)N)NC(=O)C(CCCCNC(=O)CCCCCNC(=O)C(CC(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC4=CNC5=CC=CC=C54)NC(=O)C(CC6=CC=CC=C6)NC(=O)C(CC7=CC=CC8=CC=CC=C87)NC(=O)C(CCCCN)N)NC(=O)C
CHEMBL409894 ghsr_human Human No 7.6 EC50 = 27 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
448 14 4 8 -1.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCCO)N
CHEMBL236513 ghsr_human Human No 7.6 EC50 = 27 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
480 13 3 7 0.9 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCC(=O)NCCC3=CC=CC=C3)N
CHEMBL270851 ghsr_human Human No 7.6 EC50 = 27 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
448 11 2 7 1.5 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCC(C#N)C3=CC=CC=C3)N
CHEMBL1963249 ghsr_human Human Yes 7.6 EC50 = 27 Funct
Agonist activity at ghrelin receptorAgonist activity at ghrelin receptor
539 3 3 6 3.8 CC1CNC(C(=O)N(C(C(=O)NC(C(=O)NCCCC2=CC=CC=C2O1)CC3=CC=C(C=C3)F)C)C)C4CC4
CHEMBL409894 ghsr_human Human No 7.6 EC50 = 27 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
448 14 4 8 -1.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCCO)N
CHEMBL236513 ghsr_human Human No 7.6 EC50 = 27 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
480 13 3 7 0.9 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCC(=O)NCCC3=CC=CC=C3)N
CHEMBL270851 ghsr_human Human No 7.6 EC50 = 27 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
448 11 2 7 1.5 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCC(C#N)C3=CC=CC=C3)N
CHEMBL180337 ghsr_human Human No 7.6 EC50 = 27 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
544 12 1 5 5.8 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)OCC3=CC=CC=C3)C=C(C=C2)OCC4=CC=CC=C4)C(C)C
CHEMBL2113317 ghsr_human Human No 6.6 EC50 = 279 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
525 13 3 6 3.8 COC1=CC(=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NCCN)CCC5=CC=CC=C5)OC
CHEMBL2113317 ghsr_human Human No 6.6 EC50 = 279 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
525 13 3 6 3.8 COC1=CC(=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NCCN)CCC5=CC=CC=C5)OC
CHEMBL391510 ghsr_human Human No 7.5 EC50 = 29 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 7 -0.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CC#N)N
CHEMBL3578008 ghsr_human Human No 7.5 EC50 = 29 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 10 3.3 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=CC5=CC=CC=C54)NC(=O)C(CCCCN)NC(=O)CCC(=O)O
CHEMBL391510 ghsr_human Human No 7.5 EC50 = 29 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 7 -0.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CC#N)N
CHEMBL2170781 ghsr_human Human Yes 7.5 EC50 = 29.6 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 5.9 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=CC5=CC=CC=C54)NC(=O)C(CCCCN)N
CHEMBL281764 ghsr_human Human Yes 8.5 EC50 = 3 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
529 11 2 4 4.2 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)C(CC3=CC=CC=C3)C(=O)NC)N
CHEMBL1162926 ghsr_human Human No 8.5 EC50 = 3 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
472 10 1 3 4.9 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)CC3=CC=CC=C3)NC
CHEMBL209020 ghsr_human Human No 8.5 EC50 = 3 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
506 9 2 6 1.1 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3=NN(C(=O)C3(C2)CC4=CC=CC=C4)C)N
CHEMBL1793862 ghsr_human Human No 8.5 EC50 = 3 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
479 12 4 5 2.5 CCOC(=O)C(CCC1=CC=CC=C1)NC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(C)(C)N
CHEMBL382844 ghsr_human Human No 8.5 EC50 = 3 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
492 9 3 6 1.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3=NNC(=O)C3(C2)CC4=CC=CC=C4)N
CHEMBL482420 ghsr_human Human No 8.5 EC50 = 3 Funct
Agonist activity at GHSRAgonist activity at GHSR
387 7 1 3 4.4 CC1=CC=CC=C1CN(CC2CCCN2)C(=O)C(C)OC3=CC(=CC=C3)Cl
CHEMBL409462 ghsr_human Human No 8.5 EC50 = 3 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
540 16 4 9 0.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCOC3=CC=CC(=C3)C(=O)NCCCCO)N
CHEMBL281764 ghsr_human Human Yes 8.5 EC50 = 3 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
529 11 2 4 4.2 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)C(CC3=CC=CC=C3)C(=O)NC)N
CHEMBL209020 ghsr_human Human No 8.5 EC50 = 3 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
506 9 2 6 1.1 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3=NN(C(=O)C3(C2)CC4=CC=CC=C4)C)N
CHEMBL1162058 ghsr_human Human No 8.5 EC50 = 3 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
486 11 1 3 5.4 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)CCC3=CC=CC=C3)NC
CHEMBL130229 ghsr_human Human No 8.5 EC50 = 3 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
479 12 4 5 2.5 CCOC(=O)C(CCC1=CC=CC=C1)NC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(C)(C)N
CHEMBL382844 ghsr_human Human No 8.5 EC50 = 3 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
492 9 3 6 1.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3=NNC(=O)C3(C2)CC4=CC=CC=C4)N
CHEMBL266063 ghsr_human Human No 8.5 EC50 = 3 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
602 11 4 5 4.7 COC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CCNCC5)CCC6=CNC7=CC=CC=C76
CHEMBL266063 ghsr_human Human No 8.5 EC50 = 3 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
602 11 4 5 4.7 COC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CCNCC5)CCC6=CNC7=CC=CC=C76
CHEMBL398570 ghsr_human Human No 8.5 EC50 = 3 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 13 4 9 -1.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCOC(=O)NCCO)N
CHEMBL482420 ghsr_human Human No 8.5 EC50 = 3 Funct
Agonist activity at GHSRAgonist activity at GHSR
387 7 1 3 4.4 CC1=CC=CC=C1CN(CC2CCCN2)C(=O)C(C)OC3=CC(=CC=C3)Cl
CHEMBL409462 ghsr_human Human No 8.5 EC50 = 3 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
540 16 4 9 0.7 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCOC3=CC=CC(=C3)C(=O)NCCCCO)N
CHEMBL209020 ghsr_human Human No 8.5 EC50 = 3 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
506 9 2 6 1.1 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3=NN(C(=O)C3(C2)CC4=CC=CC=C4)C)N
CHEMBL266063 ghsr_human Human No 8.5 EC50 = 3 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
602 11 4 5 4.7 COC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CCNCC5)CCC6=CNC7=CC=CC=C76
CHEMBL266063 ghsr_human Human No 8.5 EC50 = 3 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
602 11 4 5 4.7 COC1=CC=C(C=C1)CN2C(=NN=C2C(CC3=CNC4=CC=CC=C43)NC(=O)C5CCNCC5)CCC6=CNC7=CC=CC=C76
CHEMBL398570 ghsr_human Human No 8.5 EC50 = 3 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 13 4 9 -1.3 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCOC(=O)NCCO)N
CHEMBL122108 ghsr_rat Rat No 8.5 EC50 = 3 Funct
Tested for GH-releasing property using classical rat pituitary cell assayTested for GH-releasing property using classical rat pituitary cell assay
555 12 2 4 4.6 CC(C)(CC=CC(=O)N(C)C(CC1=CC=C(C=C1)C2=CC=CC=C2)C(=O)N(C)C(CC3=CC=CC=C3)C(=O)NC)N
CHEMBL281764 ghsr_human Human Yes 8.5 EC50 = 3.0 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
529 11 2 4 4.2 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)C(CC3=CC=CC=C3)C(=O)NC)N
CHEMBL1162926 ghsr_human Human No 8.5 EC50 = 3.0 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
472 10 1 3 4.9 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)CC3=CC=CC=C3)NC
CHEMBL209020 ghsr_human Human No 8.5 EC50 = 3.0 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
506 9 2 6 1.1 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3=NN(C(=O)C3(C2)CC4=CC=CC=C4)C)N
CHEMBL1793862 ghsr_human Human No 8.5 EC50 = 3.0 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
479 12 4 5 2.5 CCOC(=O)C(CCC1=CC=CC=C1)NC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(C)(C)N
CHEMBL382844 ghsr_human Human No 8.5 EC50 = 3.0 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
492 9 3 6 1.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3=NNC(=O)C3(C2)CC4=CC=CC=C4)N
CHEMBL281764 ghsr_human Human Yes 8.5 EC50 = 3.0 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
529 11 2 4 4.2 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)C(CC3=CC=CC=C3)C(=O)NC)N
CHEMBL209020 ghsr_human Human No 8.5 EC50 = 3.0 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
506 9 2 6 1.1 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3=NN(C(=O)C3(C2)CC4=CC=CC=C4)C)N
CHEMBL1162058 ghsr_human Human No 8.5 EC50 = 3.0 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
486 11 1 3 5.4 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)CCC3=CC=CC=C3)NC
CHEMBL130229 ghsr_human Human No 8.5 EC50 = 3.0 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
479 12 4 5 2.5 CCOC(=O)C(CCC1=CC=CC=C1)NC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(C)(C)N
CHEMBL382844 ghsr_human Human No 8.5 EC50 = 3.0 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
492 9 3 6 1.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3=NNC(=O)C3(C2)CC4=CC=CC=C4)N
CHEMBL281764 ghsr_human Human Yes 8.5 EC50 = 3.0 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
529 11 2 4 4.2 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)C(CC3=CC=CC=C3)C(=O)NC)N
CHEMBL1162926 ghsr_human Human No 8.5 EC50 = 3.0 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
472 10 1 3 4.9 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)CC3=CC=CC=C3)NC
CHEMBL209020 ghsr_human Human No 8.5 EC50 = 3.0 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
506 9 2 6 1.1 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3=NN(C(=O)C3(C2)CC4=CC=CC=C4)C)N
CHEMBL1793862 ghsr_human Human No 8.5 EC50 = 3.0 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
479 12 4 5 2.5 CCOC(=O)C(CCC1=CC=CC=C1)NC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(C)(C)N
CHEMBL382844 ghsr_human Human No 8.5 EC50 = 3.0 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
492 9 3 6 1.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3=NNC(=O)C3(C2)CC4=CC=CC=C4)N
CHEMBL281764 ghsr_human Human Yes 8.5 EC50 = 3.0 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
529 11 2 4 4.2 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)C(CC3=CC=CC=C3)C(=O)NC)N
CHEMBL1162058 ghsr_human Human No 8.5 EC50 = 3.0 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
486 11 1 3 5.4 CC(C)(CC=CC(=O)N(C)C(CC1=CC2=CC=CC=C2C=C1)C(=O)N(C)CCC3=CC=CC=C3)NC
CHEMBL130229 ghsr_human Human No 8.5 EC50 = 3.0 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
479 12 4 5 2.5 CCOC(=O)C(CCC1=CC=CC=C1)NC(=O)C(CC2=CNC3=CC=CC=C32)NC(=O)C(C)(C)N
CHEMBL382844 ghsr_human Human No 8.5 EC50 = 3.0 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
492 9 3 6 1.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3=NNC(=O)C3(C2)CC4=CC=CC=C4)N
CHEMBL263389 ghsr_human Human No 8.5 EC50 = 3.1 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
524 14 3 8 1.1 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)N(C)CCC3=CC(=CC=C3)O)N
CHEMBL254166 ghsr_human Human No 8.5 EC50 = 3.1 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
548 16 4 13 0.6 CC(C)(C(=O)NC(COCC1=CC(=CC=C1)OC(F)(F)F)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL263389 ghsr_human Human No 8.5 EC50 = 3.1 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
524 14 3 8 1.1 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)N(C)CCC3=CC(=CC=C3)O)N
CHEMBL254166 ghsr_human Human No 8.5 EC50 = 3.1 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
548 16 4 13 0.6 CC(C)(C(=O)NC(COCC1=CC(=CC=C1)OC(F)(F)F)C2=NN=NN2CCOC(=O)NCCCCO)N
CHEMBL400124 ghsr_human Human No 8.5 EC50 = 3.2 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
471 5 1 8 3.2 CC1CN(CCN1)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC=C(S4)C5=CC=CC=N5)OC
CHEMBL400124 ghsr_human Human No 8.5 EC50 = 3.2 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
471 5 1 8 3.2 CC1CN(CCN1)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC=C(S4)C5=CC=CC=N5)OC
CHEMBL521246 ghsr_human Human No 8.5 EC50 = 3.2 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 7 1.6 C1CCN(C(C1)C(=O)N2CCC(C2)N)S(=O)(=O)C3=CC(=C(C=C3)C4=CC=CO4)F
CHEMBL521246 ghsr_human Human No 8.5 EC50 = 3.2 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 7 1.6 C1CCN(C(C1)C(=O)N2CCC(C2)N)S(=O)(=O)C3=CC(=C(C=C3)C4=CC=CO4)F
CHEMBL2364425 ghsr_human Human No 8.5 EC50 = 3.2 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 8 4.2 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC(=C(C=C3)C4=CC=CS4)F)OC
CHEMBL2364460 ghsr_human Human No 8.5 EC50 = 3.2 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
492 6 2 7 4.7 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=C(C=C(C=C3)C4=CSC=C4)Cl
CHEMBL2364491 ghsr_human Human No 8.5 EC50 = 3.2 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 8 3.7 CC1CN(CC(N1)C)C2=CC(=C(C=C2)O)NS(=O)(=O)C3=CC(=C(C=C3)C4=CC=C(O4)C)F
CHEMBL2364485 ghsr_human Human No 8.5 EC50 = 3.2 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 8 3.1 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=NC=C(C=C3)C4=CC=C(O4)C
CHEMBL259016 ghsr_human Human No 8.5 EC50 = 3.3 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
502 14 4 8 -1.6 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCN3CCNC3=O)N
CHEMBL237701 ghsr_human Human No 8.5 EC50 = 3.3 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
503 12 3 9 -0.9 CC(=O)NC1CCN(C1)C(=O)OCCN2C(=NN=N2)C(COCC3=CC=CC=C3)NC(=O)C(C)(C)N
CHEMBL259016 ghsr_human Human No 8.5 EC50 = 3.3 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
502 14 4 8 -1.6 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCCC(=O)NCCN3CCNC3=O)N
CHEMBL237701 ghsr_human Human No 8.5 EC50 = 3.3 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
503 12 3 9 -0.9 CC(=O)NC1CCN(C1)C(=O)OCCN2C(=NN=N2)C(COCC3=CC=CC=C3)NC(=O)C(C)(C)N
CHEMBL2170781 ghsr_human Human Yes 8.5 EC50 = 3.3 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 5.9 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=CC5=CC=CC=C54)NC(=O)C(CCCCN)N
CHEMBL360877 ghsr_human Human No 8.5 EC50 = 3.4 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
542 11 1 4 6.1 CC(C)N(CCNC(=O)C1C2=C(CCN1C(=O)C(C)C3=CC=CC=C3)C=C(C=C2)OCC4=CC=CC=C4)C(C)C
CHEMBL180093 ghsr_human Human No 8.5 EC50 = 3.4 Funct
In vitro effective concentration against human growth hormone secretagoguesIn vitro effective concentration against human growth hormone secretagogues
496 12 1 5 5.2 CCCOC(=O)N1CCC2=C(C1C(=O)NCCN(C(C)C)C(C)C)C=CC(=C2)OCC3=CC=CC=C3
CHEMBL2170781 ghsr_human Human Yes 8.5 EC50 = 3.4 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 5.9 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=CC5=CC=CC=C54)NC(=O)C(CCCCN)N
CHEMBL237492 ghsr_human Human No 8.4 EC50 = 3.8 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
478 15 3 9 -0.4 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCOC(=O)N(C)CCCCO)N
CHEMBL237492 ghsr_human Human No 8.4 EC50 = 3.8 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
478 15 3 9 -0.4 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCOC(=O)N(C)CCCCO)N
CHEMBL2170781 ghsr_human Human Yes 8.4 EC50 = 3.8 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 5.9 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=CC5=CC=CC=C54)NC(=O)C(CCCCN)N
CHEMBL207970 ghsr_human Human No 8.4 EC50 = 4.0 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
520 10 2 6 1.5 CCN1C(=O)C2(CN(CCC2=N1)C(=O)C(COCC3=CC=CC=C3)NC(=O)C(C)(C)N)CC4=CC=CC=C4
CHEMBL207970 ghsr_human Human No 8.4 EC50 = 4.0 Funct
Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH releaseActivity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
520 10 2 6 1.5 CCN1C(=O)C2(CN(CCC2=N1)C(=O)C(COCC3=CC=CC=C3)NC(=O)C(C)(C)N)CC4=CC=CC=C4
CHEMBL248542 ghsr_human Human No 8.4 EC50 = 4.0 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
471 5 1 8 3.2 CC1CN(CCN1)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC=C(S4)C5=CC=CC=N5)OC
CHEMBL248542 ghsr_human Human No 8.4 EC50 = 4.0 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
471 5 1 8 3.2 CC1CN(CCN1)C2=C(C=C3CCN(C3=C2)S(=O)(=O)C4=CC=C(S4)C5=CC=CC=N5)OC
CHEMBL207970 ghsr_human Human No 8.4 EC50 = 4.0 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
520 10 2 6 1.5 CCN1C(=O)C2(CN(CCC2=N1)C(=O)C(COCC3=CC=CC=C3)NC(=O)C(C)(C)N)CC4=CC=CC=C4
CHEMBL207970 ghsr_human Human No 8.4 EC50 = 4.0 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
520 10 2 6 1.5 CCN1C(=O)C2(CN(CCC2=N1)C(=O)C(COCC3=CC=CC=C3)NC(=O)C(C)(C)N)CC4=CC=CC=C4
CHEMBL401548 ghsr_human Human No 8.4 EC50 = 4.0 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
442 6 2 7 3.5 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=CO4
CHEMBL256263 ghsr_human Human No 8.4 EC50 = 4.0 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
458 6 2 7 4.1 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=CS4
CHEMBL401548 ghsr_human Human No 8.4 EC50 = 4.0 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
442 6 2 7 3.5 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=CO4
CHEMBL256263 ghsr_human Human No 8.4 EC50 = 4.0 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
458 6 2 7 4.1 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=CS4
CHEMBL1079186 ghsr_human Human No 8.4 EC50 = 4.0 Funct
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
453 8 2 5 4.7 CCCCC1=CC=C(C=C1)S(=O)(=O)NC2=CC3=C(CCN(CC3)CC4=C(NC=N4)C)C=C2
CHEMBL1079185 ghsr_human Human No 8.4 EC50 = 4.0 Funct
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
439 8 2 5 4.3 CCCCC1=CC=C(C=C1)S(=O)(=O)NC2=CC3=C(CCN(CC3)CC4=CN=CN4)C=C2
CHEMBL1079186 ghsr_human Human No 8.4 EC50 = 4.0 Funct
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
453 8 2 5 4.7 CCCCC1=CC=C(C=C1)S(=O)(=O)NC2=CC3=C(CCN(CC3)CC4=C(NC=N4)C)C=C2
CHEMBL1079185 ghsr_human Human No 8.4 EC50 = 4.0 Funct
Agonist activity at human ghrelin receptorAgonist activity at human ghrelin receptor
439 8 2 5 4.3 CCCCC1=CC=C(C=C1)S(=O)(=O)NC2=CC3=C(CCN(CC3)CC4=CN=CN4)C=C2
CHEMBL519121 ghsr_human Human No 8.4 EC50 = 4.0 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
475 5 2 7 1.7 C1CCN(C(C1)C(=O)N2CCC(C2)N)S(=O)(=O)C3=CC=C(C=C3)NC(=O)C4=CC=CC=C4F
CHEMBL519121 ghsr_human Human No 8.4 EC50 = 4.0 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
475 5 2 7 1.7 C1CCN(C(C1)C(=O)N2CCC(C2)N)S(=O)(=O)C3=CC=C(C=C3)NC(=O)C4=CC=CC=C4F
CHEMBL2364473 ghsr_human Human No 8.4 EC50 = 4.0 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
490 6 2 8 4.6 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC(=C(C=C3)C4=CC=C(S4)C)F
CHEMBL2364413 ghsr_human Human No 8.4 EC50 = 4.0 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 4.8 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(S3)C4=CC(=CC=C4)C)OC
CHEMBL2364459 ghsr_human Human No 8.4 EC50 = 4.0 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
490 6 2 8 4.6 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=C(C=C(C=C3)C4=CC=C(S4)C)F
CHEMBL2364423 ghsr_human Human No 8.4 EC50 = 4.0 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 5 2 6 4.5 CC1CN(CC(N1)C)C2=CC(=C(C=C2)C)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=CS4
CHEMBL2364374 ghsr_human Human No 8.4 EC50 = 4.0 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
464 6 2 8 4.1 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(S3)C4=CC=CS4
CHEMBL2364482 ghsr_human Human No 8.4 EC50 = 4.0 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 4.5 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CSC(=C4)C
CHEMBL236038 ghsr_human Human No 7.5 EC50 = 30 Funct
Agonist activity at GHS receptorAgonist activity at GHS receptor
357 9 2 7 -0.6 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCC#N)N
CHEMBL489401 ghsr_human Human No 7.5 EC50 = 30 Funct
Agonist activity at GHSRAgonist activity at GHSR
416 7 2 4 3.3 CC(C(=O)N(CC1CCCN1)C2=CC=C(C=C2)NC(=O)C)OC3=CC(=CC=C3)Cl
CHEMBL521176 ghsr_human Human No 7.5 EC50 = 30 Funct
Agonist activity at GHSRAgonist activity at GHSR
407 7 1 3 4.7 CC(C(=O)N(CC1CCCN1)CC2=CC=C(C=C2)Cl)OC3=CC(=CC=C3)Cl
CHEMBL236311 ghsr_human Human No 7.5 EC50 = 30 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
446 14 3 7 0.6 CCCCNC(=O)CCCN1C(=NN=N1)C(COCC2=CC=CC=C2)NC(=O)C(C)(C)N
CHEMBL236038 ghsr_human Human No 7.5 EC50 = 30 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 7 -0.6 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCC#N)N
CHEMBL236311 ghsr_human Human No 7.5 EC50 = 30 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
446 14 3 7 0.6 CCCCNC(=O)CCCN1C(=NN=N1)C(COCC2=CC=CC=C2)NC(=O)C(C)(C)N
CHEMBL608827 ghsr_human Human No 7.5 EC50 = 30 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
608 9 1 8 4.5 CCN(CC)CCN1C2=CC(=CC(=C2C(C1=O)(C3=CC4=CC=CC=C4C=C3)O)C(F)(F)F)C#CCCC(=O)N5CCOCC5
CHEMBL611488 ghsr_human Human No 7.5 EC50 = 30 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
566 9 1 7 4.9 CCN(CC)CCN1C2=CC(=CC(=C2C(C1=O)(C3=CC4=CC=CC=C4C=C3)O)C(F)(F)F)C#CCCC(=O)N(C)C
CHEMBL236038 ghsr_human Human No 7.5 EC50 = 30 Funct
Agonist activity at GHS receptorAgonist activity at GHS receptor
357 9 2 7 -0.6 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCC#N)N
CHEMBL489401 ghsr_human Human No 7.5 EC50 = 30 Funct
Agonist activity at GHSRAgonist activity at GHSR
416 7 2 4 3.3 CC(C(=O)N(CC1CCCN1)C2=CC=C(C=C2)NC(=O)C)OC3=CC(=CC=C3)Cl
CHEMBL521176 ghsr_human Human No 7.5 EC50 = 30 Funct
Agonist activity at GHSRAgonist activity at GHSR
407 7 1 3 4.7 CC(C(=O)N(CC1CCCN1)CC2=CC=C(C=C2)Cl)OC3=CC(=CC=C3)Cl
CHEMBL236311 ghsr_human Human No 7.5 EC50 = 30 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
446 14 3 7 0.6 CCCCNC(=O)CCCN1C(=NN=N1)C(COCC2=CC=CC=C2)NC(=O)C(C)(C)N
CHEMBL236038 ghsr_human Human No 7.5 EC50 = 30 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 7 -0.6 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN=NN2CCC#N)N
CHEMBL236311 ghsr_human Human No 7.5 EC50 = 30 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
446 14 3 7 0.6 CCCCNC(=O)CCCN1C(=NN=N1)C(COCC2=CC=CC=C2)NC(=O)C(C)(C)N
CHEMBL608827 ghsr_human Human No 7.5 EC50 = 30 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
608 9 1 8 4.5 CCN(CC)CCN1C2=CC(=CC(=C2C(C1=O)(C3=CC4=CC=CC=C4C=C3)O)C(F)(F)F)C#CCCC(=O)N5CCOCC5
CHEMBL608827 ghsr_human Human No 7.5 EC50 = 30.2 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
608 9 1 8 4.5 CCN(CC)CCN1C2=CC(=CC(=C2C(C1=O)(C3=CC4=CC=CC=C4C=C3)O)C(F)(F)F)C#CCCC(=O)N5CCOCC5
CHEMBL611488 ghsr_human Human No 7.5 EC50 = 30.2 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
566 9 1 7 4.9 CCN(CC)CCN1C2=CC(=CC(=C2C(C1=O)(C3=CC4=CC=CC=C4C=C3)O)C(F)(F)F)C#CCCC(=O)N(C)C
CHEMBL611488 ghsr_human Human No 7.5 EC50 = 30.2 Funct
Agonist activity at human GHS-R1Agonist activity at human GHS-R1
566 9 1 7 4.9 CCN(CC)CCN1C2=CC(=CC(=C2C(C1=O)(C3=CC4=CC=CC=C4C=C3)O)C(F)(F)F)C#CCCC(=O)N(C)C
CHEMBL256236 ghsr_human Human No 6.5 EC50 = 302 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
448 11 2 7 2.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN(N=N2)CCC(C#N)C3=CC=CC=C3)N
CHEMBL256236 ghsr_human Human No 6.5 EC50 = 302 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
448 11 2 7 2.0 CC(C)(C(=O)NC(COCC1=CC=CC=C1)C2=NN(N=N2)CCC(C#N)C3=CC=CC=C3)N
CHEMBL401133 ghsr_human Human No 7.5 EC50 = 31.6 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
541 5 1 6 3.6 CC1CN(CC(N1)C)C2=C(C=C3CCN(C3=C2)S(=O)(=O)CC4=CC(=CC=C4)I)OC
CHEMBL481602 ghsr_human Human No 7.5 EC50 = 31.6 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 6 1.5 C1CCN(C(C1)C(=O)N2CCC(C2)N)S(=O)(=O)C3=CC=C(C=C3)C4=CC=CO4
CHEMBL517081 ghsr_human Human No 7.5 EC50 = 31.6 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
414 4 1 5 2.4 C1CCN(C(C1)C(=O)N2CCC(C2)N)S(=O)(=O)C3=CC=C(C=C3)C4=CC=CC=C4
CHEMBL3578008 ghsr_human Human No 7.5 EC50 = 31.6 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 10 3.3 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=CC5=CC=CC=C54)NC(=O)C(CCCCN)NC(=O)CCC(=O)O
CHEMBL401133 ghsr_human Human No 7.5 EC50 = 31.6 Funct
Agonist activity at GSHR by FLIPR assayAgonist activity at GSHR by FLIPR assay
541 5 1 6 3.6 CC1CN(CC(N1)C)C2=C(C=C3CCN(C3=C2)S(=O)(=O)CC4=CC(=CC=C4)I)OC
CHEMBL481602 ghsr_human Human No 7.5 EC50 = 31.6 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 6 1.5 C1CCN(C(C1)C(=O)N2CCC(C2)N)S(=O)(=O)C3=CC=C(C=C3)C4=CC=CO4
CHEMBL517081 ghsr_human Human No 7.5 EC50 = 31.6 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
414 4 1 5 2.4 C1CCN(C(C1)C(=O)N2CCC(C2)N)S(=O)(=O)C3=CC=C(C=C3)C4=CC=CC=C4
CHEMBL3578008 ghsr_human Human No 7.5 EC50 = 31.6 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 10 3.3 CC(C)CC(C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC4=CC=CC5=CC=CC=C54)NC(=O)C(CCCCN)NC(=O)CCC(=O)O
CHEMBL2364347 ghsr_human Human No 7.5 EC50 = 31.6 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
426 5 2 6 4.0 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=CC4=CC=CC=C43)OC
CHEMBL2364405 ghsr_human Human No 7.5 EC50 = 31.6 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
488 6 2 8 4.6 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(C=C3)C4=C(C(=CC=C4)F)F)OC
CHEMBL2364394 ghsr_human Human No 7.5 EC50 = 31.6 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
402 4 2 6 4.1 CC1CN(CC(N1)C)C2=CC(=CC=C2)NS(=O)(=O)C3=CC4=CC=CC=C4S3
CHEMBL2364453 ghsr_human Human No 7.5 EC50 = 31.6 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 2 7 3.7 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC4=C(C=C3)OC(CC4)(C)C
CHEMBL2364416 ghsr_human Human No 7.5 EC50 = 31.6 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 8 4.5 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(S3)C4=CC(=CC=C4)F
CHEMBL2364417 ghsr_human Human No 7.5 EC50 = 31.6 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 4.8 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(S3)C4=CC=C(C=C4)C
CHEMBL2364436 ghsr_human Human No 7.5 EC50 = 31.6 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
488 6 2 8 4.6 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=C(C(=CC=C4)F)F
CHEMBL2364378 ghsr_human Human No 7.5 EC50 = 31.6 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
464 5 2 8 4.6 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=C(C4=C(S3)C=CC(=C4)F)C
CHEMBL2364439 ghsr_human Human No 7.5 EC50 = 31.6 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
440 5 2 6 4.5 CC1CN(CC(N1)C)C2=CC(=C(C=C2)F)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=CC=C4
CHEMBL2364345 ghsr_human Human No 7.5 EC50 = 31.6 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
480 5 2 7 5.1 CC1CN(CC(N1)C)C2=C(C=CC(=C2)NS(=O)(=O)C3=C(C4=C(S3)C=CC(=C4)Cl)C)OC
CHEMBL2364446 ghsr_human Human No 7.5 EC50 = 31.6 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 7 3.9 CC1CN(CC(N1)C)C2=CC(=C(C=C2)F)NS(=O)(=O)C3=C(C=C(C=C3)C4=COC=C4)C
CHEMBL2364386 ghsr_human Human No 7.5 EC50 = 31.6 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 7 2 9 3.3 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(S3)C4=C(C=CN=C4)OC
CHEMBL2364339 ghsr_human Human No 7.5 EC50 = 31.6 Funct
SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945SUPPLEMENTARY: Agonist activity at GSHR by FLIPR assay. Same assay as CHEMBL941945
446 5 2 9 3.0 CC1CN(CC(N1)C)C2=NC=CC(=N2)NS(=O)(=O)C3=CC(=C(C=C3)C4=CC=C(O4)C)F
CHEMBL2364467 ghsr_human Human No 7.5 EC50 = 31.6 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 8 2.3 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=NC=CN=C4
CHEMBL2364490 ghsr_human Human No 7.5 EC50 = 31.6 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 6 2 7 3.7 CC1CN(CCN1)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=CS4
CHEMBL255401 ghsr_human Human No 6.5 EC50 = 316.2 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
454 6 2 8 2.7 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CN=CN=C4
CHEMBL401891 ghsr_human Human No 6.5 EC50 = 316.2 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
453 6 2 7 3.3 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=NC=C4
CHEMBL479865 ghsr_human Human No 6.5 EC50 = 316.2 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
415 4 1 6 1.3 C1CCN(C(C1)C(=O)N2CCC(C2)N)S(=O)(=O)C3=CC=C(C=C3)C4=CN=CC=C4
CHEMBL3578013 ghsr_human Human No 6.5 EC50 = 316.2 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
2872 96 41 34 0.6 CC(C)CC(C(=O)NC(CCCNC(=N)N)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)O)C(=O)NC(CC(C)C)C(=O)NC(CC(=O)N)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(C(C)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC3=CC=C(C=C3)O)C(=O)N)NC(=O)C(CCCCNC(=O)CCNC(=O)C(CC(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC4=CNC5=CC=CC=C54)NC(=O)C(CC6=CC=CC=C6)NC(=O)C(CC7=CC=CC8=CC=CC=C87)NC(=O)C(CCCCN)N)NC(=O)C
CHEMBL255401 ghsr_human Human No 6.5 EC50 = 316.2 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
454 6 2 8 2.7 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CN=CN=C4
CHEMBL401891 ghsr_human Human No 6.5 EC50 = 316.2 Funct
Agonist activity at human GHSR1a by FLIPR assayAgonist activity at human GHSR1a by FLIPR assay
453 6 2 7 3.3 CC1CN(CC(N1)C)C2=CC(=C(C=C2)OC)NS(=O)(=O)C3=CC=C(C=C3)C4=CC=NC=C4
CHEMBL479865 ghsr_human Human No 6.5 EC50 = 316.2 Funct
Agonist activity at human ghrelin receptor by cell based BACMAM FLIPR assayAgonist activity at human ghrelin receptor by cell based BACMAM FLIPR assay
415 4 1 6 1.3 C1CCN(C(C1)C(=O)N2CCC(C2)N)S(=O)(=O)C3=CC=C(C=C3)C4=CN=CC=C4
CHEMBL3578013 ghsr_human Human No 6.5 EC50 = 316.2 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
2872 96 41 34 0.6 CC(C)CC(C(=O)NC(CCCNC(=N)N)C(=O)NC(CC1=CN=CN1)C(=O)NC(CC2=CC=C(C=C2)O)C(=O)NC(CC(C)C)C(=O)NC(CC(=O)N)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(C(C)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC3=CC=C(C=C3)O)C(=O)N)NC(=O)C(CCCCNC(=O)CCNC(=O)C(CC(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC4=CNC5=CC=CC=C54)NC(=O)C(CC6=CC=CC=C6)NC(=O)C(CC7=CC=CC8=CC=CC=C87)NC(=O)C(CCCCN)N)NC(=O)C